MA33726B1 - Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation - Google Patents
Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisationInfo
- Publication number
- MA33726B1 MA33726B1 MA34836A MA34836A MA33726B1 MA 33726 B1 MA33726 B1 MA 33726B1 MA 34836 A MA34836 A MA 34836A MA 34836 A MA34836 A MA 34836A MA 33726 B1 MA33726 B1 MA 33726B1
- Authority
- MA
- Morocco
- Prior art keywords
- compounds
- dioxide compounds
- iminotiadiazine
- formulations
- stereoisomers
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- A61K31/549—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 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
-
- 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
-
- 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
- A61P27/00—Drugs for disorders of the senses
-
- 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
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- 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
- C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/15—Six-membered rings
- C07D285/16—Thiadiazines; Hydrogenated thiadiazines
- C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D417/10—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 linked by a carbon chain containing aromatic 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
- A61K31/495—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
-
- 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
- C07D213/24—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 with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/26—Radicals substituted by halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/12—Nitrogen atoms not forming part of a nitro radical
- C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Otolaryngology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
Abstract
Dans ses nombreux modes de réalisation, la présente invention concerne certains composés de dioxyde d'iminothiadiazine, notamment des composés de formule (I): (I) et comprend leurs stéréo-isomères, et les sels pharmaceutiquement acceptables desdits stéréo-isomères des composés, chacun parmi R1, R2, R3, R4, R5, R9, cycle A, cycle B, m, n, p, -L1-,L2-, et L3- étant indépendamment choisi et tel que défini ici. Etonnamment, les nouveaux composés de dioxyde d'iminothiadiazine de l'invention se sont révélés présenter des propriétés qui font espérer qu'elles les rendront avantageux en tant qu'inhibiteurs de BACE et/ou pour le traitement et la prévention de diverses pathologies liées à la production de ²-amyloïde (A²). L'invention concerne également des compositions pharmaceutiques comprenant un ou plusieurs de ces composés (seuls et en combinaison avec un ou plusieurs autres agents actifs), et des procédés pour leur préparation et leur utilisation dans le traitement de pathologies associées à la protéine amyloïde bêta (A²), notamment la maladie d'Alzheimer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US24968509P | 2009-10-08 | 2009-10-08 | |
PCT/US2010/051553 WO2011044181A1 (fr) | 2009-10-08 | 2010-10-06 | Composés de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utilisation |
Publications (1)
Publication Number | Publication Date |
---|---|
MA33726B1 true MA33726B1 (fr) | 2012-11-01 |
Family
ID=43857101
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MA34836A MA33726B1 (fr) | 2009-10-08 | 2012-05-04 | Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation |
Country Status (39)
Country | Link |
---|---|
US (6) | US8729071B2 (fr) |
EP (2) | EP2485736B1 (fr) |
JP (4) | JP5592494B2 (fr) |
KR (3) | KR101646424B1 (fr) |
CN (2) | CN104744403A (fr) |
AR (1) | AR078534A1 (fr) |
AU (1) | AU2010303591B2 (fr) |
BR (1) | BR112012008014B1 (fr) |
CA (1) | CA2774579C (fr) |
CL (1) | CL2012000872A1 (fr) |
CR (1) | CR20120158A (fr) |
DK (1) | DK2485736T3 (fr) |
DO (1) | DOP2012000067A (fr) |
EA (1) | EA025120B1 (fr) |
EC (1) | ECSP12011857A (fr) |
ES (2) | ES2773908T3 (fr) |
GE (1) | GEP20156366B (fr) |
HK (2) | HK1167608A1 (fr) |
HN (1) | HN2012000612A (fr) |
HR (1) | HRP20160185T1 (fr) |
HU (1) | HUE028672T2 (fr) |
IL (3) | IL218712A (fr) |
MA (1) | MA33726B1 (fr) |
ME (1) | ME02366B (fr) |
MX (1) | MX2012004148A (fr) |
MY (1) | MY163744A (fr) |
NI (1) | NI201200044A (fr) |
NZ (1) | NZ598694A (fr) |
PE (1) | PE20141935A1 (fr) |
PL (1) | PL2485736T3 (fr) |
PT (1) | PT2485736E (fr) |
RS (1) | RS54587B1 (fr) |
SG (1) | SG10201406365WA (fr) |
SI (1) | SI2485736T1 (fr) |
TN (1) | TN2012000112A1 (fr) |
TW (3) | TWI477502B (fr) |
UA (1) | UA108363C2 (fr) |
WO (1) | WO2011044181A1 (fr) |
ZA (2) | ZA201202517B (fr) |
Families Citing this family (127)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
EP2147914B1 (fr) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Dérivés d'aminodihydrothiazine substitués par des groupes cycliques |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
EP2485590B1 (fr) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Composés hétérocycliques de type imino-pentafluorosulfure utilisés en tant qu'inhibiteurs de bace1, compositions en contenant et leur utilisation |
US8569310B2 (en) * | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
EP2485591B1 (fr) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Composés de type dioxyde d'imino-thiadiazine utilisés en tant qu'inhibiteurs de bace, compositions en contenant et leur utilisation |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
US8404680B2 (en) | 2011-02-08 | 2013-03-26 | Hoffmann-La Roche Inc. | N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors |
WO2012138734A1 (fr) * | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Composés de dioxyde de thiadiazine condensés avec des dérivés oxacycliques en c5-c6 comme inhibiteurs de bace, compositions, et utilisation use |
US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
MX2013011947A (es) | 2011-04-13 | 2014-01-16 | Merck Sharp & Dohme | Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso. |
US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
CN103649082A (zh) | 2011-04-26 | 2014-03-19 | 盐野义制药株式会社 | 吡啶衍生物和含有该吡啶衍生物的bace1抑制剂 |
US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
CA2858157A1 (fr) * | 2011-12-06 | 2013-06-13 | Ube Industries, Ltd. | Procede pour la production d'acide pentafluorosulfanylbenzoique |
MX354173B (es) | 2012-01-26 | 2018-02-16 | Hoffmann La Roche | Fluorometil-5,6-dihidro-4h-[1,3]oxazinas. |
BR112014026176A2 (pt) * | 2012-05-22 | 2017-06-27 | Hoffmann La Roche | dipiridilaminas substituídas e usos das mesmas |
EP2908824B1 (fr) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Composés de dioxyde de thiadiazine substituée tricyclique utilisés en tant qu'inhibiteurs de bace, compositions et leur utilisation |
US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
WO2014065434A1 (fr) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dérivés de dihydrooxazine ou d'oxazépine ayant une activité inhibitrice de bace1 |
US8865723B2 (en) | 2012-10-25 | 2014-10-21 | Tetra Discovery Partners Llc | Selective PDE4 B inhibition and improvement in cognition in subjects with brain injury |
US9447085B2 (en) | 2012-12-14 | 2016-09-20 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use |
US9489013B2 (en) | 2012-12-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
WO2014099768A1 (fr) * | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Dioxydes d'azaspiro-iminothiadiazine en c6 pouvant être utilisés en tant qu'inhibiteurs de bace |
US9365589B2 (en) | 2012-12-20 | 2016-06-14 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused thiazine dioxide compounds as BACE inhibitors, compositions, and their use |
WO2014099788A1 (fr) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | Dioxydes d'iminothiadiazine spiro c5 utilisés en tant qu'inhibiteurs de bace |
CN107412788B (zh) | 2012-12-21 | 2021-06-18 | 国立研究开发法人量子科学技术研究开发机构 | 用于对脑内所蓄积的Tau蛋白质进行成像的新的化合物 |
KR102220259B1 (ko) | 2013-02-12 | 2021-02-25 | 버크 인스티튜트 포 리서치 온 에이징 | Bace 매개 app 처리과정을 조절하는 히단토인 |
WO2014134341A1 (fr) | 2013-03-01 | 2014-09-04 | Amgen Inc. | Composés perfluorés 5,6-dihydro-4h-1,3-oxazine-2-amine substitués en tant qu'inhibiteurs de la bêta-sécrétase et procédés d'utilisation correspondants |
SG11201507196WA (en) | 2013-03-08 | 2015-10-29 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
EP2968356B1 (fr) * | 2013-03-15 | 2018-03-07 | Merck Sharp & Dohme Corp. | Composés s-imino-s-oxo iminothiadiazine servant d'inhibiteurs de l'enzyme de clivage du site ss de l'app, compositions, et leur utilisation |
WO2014150331A1 (fr) * | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | Composés s-imino-s-oxo iminothiazine servant d'inhibiteurs de l'enzyme de clivage du site ss de l'app, compositions, et leur utilisation |
EP2968353B1 (fr) | 2013-03-15 | 2018-12-19 | Merck Sharp & Dohme Corp. | Dioxydes c2-azaspiro iminothiazines en tant qu'inhibiteurs de bace |
CN103214413B (zh) * | 2013-03-22 | 2015-05-13 | 郑州泰基鸿诺药物科技有限公司 | 一种含杂环的三氟甲基酮化合物及其制备方法 |
RU2015147601A (ru) | 2013-05-01 | 2017-06-05 | Ф. Хоффманн-Ля Рош Аг | С-связанные гетероциклоалкилзамещенные пиримидины и их применения |
LT3049417T (lt) * | 2013-07-31 | 2019-02-11 | Merck Patent Gmbh | Piridinai, pirimidnai ir pirazinai kaip btk inhibitoriai ir jų panaudojimas |
EP3083575B1 (fr) * | 2013-12-18 | 2021-11-03 | Merck Sharp & Dohme Corp. | Dioxides d'iminothiadiazine spirocarbocyclique c-6 servant d'inhibiteurs de bace, compositions, et leur utilisation |
EP3082823B1 (fr) | 2013-12-18 | 2020-04-22 | Merck Sharp & Dohme Corp. | Composés de dioxyde d'iminothiadiazépane utilisés en tant qu'inhibiteurs de bace, compositions et leur utilisation |
CN106132950B (zh) | 2014-01-01 | 2018-11-09 | 麦迪威森技术有限责任公司 | 氨基吡啶类化合物和使用方法 |
CN103910781B (zh) * | 2014-03-18 | 2016-02-17 | 重庆大学 | 一种Aβ聚集抑制剂 |
CA2944971C (fr) | 2014-04-10 | 2019-05-07 | Pfizer Inc. | Amides 2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8h)-yl-1,3-thiazol-4-yle |
CN103880757B (zh) * | 2014-04-15 | 2016-02-24 | 上海毕得医药科技有限公司 | 一种5-羟基嘧啶-2-羧酸的合成方法 |
MX2017001794A (es) | 2014-08-08 | 2017-06-29 | Amgen Inc | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
US20170233382A1 (en) * | 2014-08-14 | 2017-08-17 | Merck Sharp & Dohme Corp. | Processes for the preparation of a bace inhibitor |
US10035796B2 (en) | 2014-08-14 | 2018-07-31 | Merck Sharp & Dohme Corp. | Crystalline forms of a BACE inhibitor, compositions, and their use |
CA2952160A1 (fr) * | 2014-08-15 | 2016-02-18 | F. Hoffmann-La Roche Ag | 2,2,2-trifluoroethyl-thiadiazines |
EP3191447B1 (fr) * | 2014-09-12 | 2019-05-01 | Merck Sharp & Dohme Corp. | Composés de s-imino-s-oxo iminothiazine en tant qu'inhibiteurs de bace, compositions, et leur utilisation |
WO2016044120A1 (fr) | 2014-09-19 | 2016-03-24 | Merck Sharp & Dohme Corp. | Composés d'amidine à diazine fusionnée utilisés en tant qu'inhibiteurs de bace, compositions et leur utilisation |
WO2016053767A1 (fr) * | 2014-09-30 | 2016-04-07 | Merck Sharp & Dohme Corp. | Nouvelles formes cristallines d'un inhibiteur de bace, compositions, et utilisation associées |
US10238743B2 (en) | 2014-10-03 | 2019-03-26 | Merck Sharp & Dohme Corp. | C5-C6-fused tricyclic iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
EP3223820B1 (fr) | 2014-11-25 | 2020-07-22 | Merck Sharp & Dohme Corp. | Composés de 3-methyl-2-imino-hexahydro-1h-pyrano[3,4-d]pyrimidin-4-one utilisés comme inhibiteurs de bace, compositions et utilisation associées |
WO2016118404A1 (fr) | 2015-01-20 | 2016-07-28 | Merck Sharp & Dohme Corp. | Dioxydes d'iminothiadiazine portant un substituant lié à une amine, utilisés en tant qu'inhibiteurs de bace, compositions les contenant et leur utilisation |
CA2979905A1 (fr) * | 2015-04-21 | 2016-10-27 | Allgenesis Biotherapeutics, Inc. | Composes et leur utilisation en tant qu'inhibiteurs de bace1 |
BR112018003489A2 (pt) | 2015-09-24 | 2018-09-25 | Pfizer | n-[2-(2-amino-6,6-dissubstituído-4,4a,5,6-tetra-hidropirano[3,4-d][1,3]tiazin-8a(8h)-il)-1,3-tiazol-4-il]amidas |
JP2018531924A (ja) | 2015-09-24 | 2018-11-01 | ファイザー・インク | テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用 |
WO2017051294A1 (fr) * | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(3-amino-2,5-diméthyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides utiles comme inhibiteurs de bace |
TW201718581A (zh) | 2015-10-19 | 2017-06-01 | 英塞特公司 | 作為免疫調節劑之雜環化合物 |
CN105218425A (zh) * | 2015-10-31 | 2016-01-06 | 丁玉琴 | 一种3,5-二甲氧基吡咯-2-甲酸的合成方法 |
LT3377488T (lt) | 2015-11-19 | 2023-01-10 | Incyte Corporation | Heterocikliniai junginiai, kaip imunomoduliatoriai |
US10329291B2 (en) | 2015-12-04 | 2019-06-25 | Merck Sharp & Dohme Corp. | C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
WO2017106634A1 (fr) * | 2015-12-17 | 2017-06-22 | Incyte Corporation | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation comme modulateurs d'interactions protéine/protéine pd-1/pd-l1 |
SI3394033T1 (sl) | 2015-12-22 | 2021-03-31 | Incyte Corporation | Heterociklične spojine kot imunomodulatorji |
US10604534B2 (en) | 2016-02-11 | 2020-03-31 | Merck Sharp & Dohme Corp. | C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use |
EP3416648A4 (fr) * | 2016-02-17 | 2019-09-18 | Merck Sharp & Dohme Corp. | Procédés de préparation d'inhibiteurs de bace |
GB201603104D0 (en) * | 2016-02-23 | 2016-04-06 | Ucb Biopharma Sprl | Therapeutic agents |
MA44860A (fr) | 2016-05-06 | 2019-03-13 | Incyte Holdings Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
WO2017205464A1 (fr) | 2016-05-26 | 2017-11-30 | Incyte Corporation | Composés hétérocycliques utilisés comme immunomodulateurs |
EP4137489A1 (fr) | 2016-06-20 | 2023-02-22 | Incyte Corporation | Composés hétérocycliques en tant qu'immunomodulateurs |
TWI735600B (zh) | 2016-07-01 | 2021-08-11 | 美商美國禮來大藥廠 | 抗-N3pGlu類澱粉β肽抗體及其用途 |
WO2018013789A1 (fr) | 2016-07-14 | 2018-01-18 | Incyte Corporation | Composés hétérocycliques utilisés comme immunomodulateurs |
EP3504198B1 (fr) | 2016-08-29 | 2023-01-25 | Incyte Corporation | Composés hétérocycliques utilisés comme immunomodulateurs |
MX2019007104A (es) * | 2016-12-15 | 2019-11-05 | Amgen Inc | Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. |
JP7149272B2 (ja) | 2016-12-15 | 2022-10-06 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としてのチアジン誘導体および使用方法 |
US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
JP7159161B2 (ja) | 2016-12-15 | 2022-10-24 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としてのシクロプロピル縮合チアジン誘導体および使用方法 |
US11548903B2 (en) | 2016-12-15 | 2023-01-10 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
US20180179179A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
TWI798192B (zh) | 2016-12-22 | 2023-04-11 | 美商英塞特公司 | 免疫調節劑化合物及使用方法 |
MX2019007416A (es) | 2016-12-22 | 2019-12-11 | Incyte Corp | Derivados de benzooxazol como inmunomoduladores. |
EP3372599A1 (fr) | 2017-03-07 | 2018-09-12 | Sandoz AG | Forme cristalline de verubecestat |
US20200080154A1 (en) * | 2017-05-02 | 2020-03-12 | Sanford Burnham Prebys Medical Discovery Institute | Methods of diagnosing and treating alzheimer's disease |
WO2018202524A1 (fr) | 2017-05-04 | 2018-11-08 | Bayer Cropscience Aktiengesellschaft | Dérivés de 2-{[2-(phényloxyméthyl)pyridin-5-yl]oxy}-éthanamine et composés apparentés utilisés comme pesticides, par exemple pour la protection des plantes |
WO2018231634A1 (fr) | 2017-06-13 | 2018-12-20 | Merck Sharp & Dohme Corp. | Nouvelle forme cristalline d'un inhibiteur de bace, compositions, et utilisation |
ES2940750T3 (es) | 2018-03-30 | 2023-05-11 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
GB201805816D0 (en) * | 2018-04-06 | 2018-05-23 | Ucb Biopharma Sprl | Therapeutic agents |
JP2022511167A (ja) * | 2018-04-23 | 2022-01-31 | 塩野義製薬株式会社 | 選択的bace1阻害活性を有する二環式複素環誘導体 |
BR112020021728A2 (pt) | 2018-04-27 | 2021-01-26 | Shionogi & Co., Ltd. | derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva |
US12116364B2 (en) * | 2018-05-09 | 2024-10-15 | Aprinoia Therapeutics Inc. | Heteroaryl compounds and uses thereof |
HRP20230306T1 (hr) | 2018-05-11 | 2023-05-12 | Incyte Corporation | Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori |
CN110467611B (zh) * | 2018-05-11 | 2022-09-27 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN108863983B (zh) * | 2018-08-03 | 2020-01-21 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN108997328B (zh) * | 2018-09-06 | 2021-06-08 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN109180669B (zh) * | 2018-09-06 | 2022-05-27 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN109180670A (zh) * | 2018-09-17 | 2019-01-11 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN109180671A (zh) * | 2018-09-21 | 2019-01-11 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN109180672A (zh) * | 2018-09-29 | 2019-01-11 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
CN109796447B (zh) * | 2019-01-07 | 2020-03-13 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
GB201906804D0 (en) | 2019-05-14 | 2019-06-26 | Ucb Biopharma Sprl | Therapeutic agents |
CA3150434A1 (fr) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Sels d'un inhibiteur de pd-1/pd-l1 |
WO2021026884A1 (fr) * | 2019-08-15 | 2021-02-18 | Merck Sharp & Dohme Corp. | Agents antipaludiques |
CN114206856A (zh) * | 2019-08-19 | 2022-03-18 | Ucb生物制药有限责任公司 | 抗疟疾的六氢嘧啶类似物 |
TW202126652A (zh) | 2019-09-30 | 2021-07-16 | 美商英塞特公司 | 作為免疫調節劑之吡啶并[3,2—d]嘧啶化合物 |
KR20220101664A (ko) | 2019-11-11 | 2022-07-19 | 인사이트 코포레이션 | Pd-1/pd-l1 억제제의 염 및 결정질 형태 |
CA3161455A1 (fr) | 2019-11-13 | 2021-05-20 | Aprinoia Therapeutics Limited | Composes pour degrader des agregats de proteine tau et leurs utilisations |
JPWO2021117759A1 (fr) | 2019-12-10 | 2021-06-17 | ||
CN113087669B (zh) * | 2019-12-23 | 2023-11-17 | 南京药石科技股份有限公司 | 一种4-氰基-5-溴嘧啶的制备方法 |
WO2021155612A1 (fr) * | 2020-02-09 | 2021-08-12 | Merck Sharp & Dohme Corp. | Agents antipaludiques |
WO2021195403A1 (fr) | 2020-03-26 | 2021-09-30 | Cyclerion Therapeutics, Inc. | Stimulateurs de sgc deutérés |
MX2023000167A (es) * | 2020-07-02 | 2023-05-03 | Remix Therapeutics Inc | Derivados de 5-[5-(piperidin-4-il)tieno[3,2-c]pirazol-2-il]indazol y compuestos relacionados como moduladores para el corte y empalme de ácidos nucleicos y para el tratamiento de enfermedades proliferativas. |
GB202010606D0 (en) | 2020-07-10 | 2020-08-26 | Ucb Biopharma Sprl | Therapeutic agents |
WO2023102747A1 (fr) * | 2021-12-07 | 2023-06-15 | Merck Sharp & Dohme Llc | Agents antipaludiques |
WO2022099018A1 (fr) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Procédé de préparation d'un inhibiteur de pd-1/pd-l1 |
US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
US11866434B2 (en) | 2020-11-06 | 2024-01-09 | Incyte Corporation | Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof |
EP4294781A1 (fr) | 2021-02-22 | 2023-12-27 | Solvay SA | Procédé catalytique pour la préparation d'arènes et hétéroarènes substitués par perfluoroalcoxy |
CN113880755B (zh) * | 2021-08-27 | 2024-06-18 | 成都药明康德新药开发有限公司 | 2-溴-5-(三氟甲氧基)吡啶的制备方法 |
WO2023133229A2 (fr) * | 2022-01-05 | 2023-07-13 | Remix Therapeutics Inc. | Composés et procédés de modulation d'épissage |
CN118085013A (zh) * | 2022-11-25 | 2024-05-28 | 成都微芯新域生物技术有限公司 | 一种连接子、含连接子的抗体药物偶联物及其制备方法和应用 |
Family Cites Families (170)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4863936A (en) * | 1982-12-14 | 1989-09-05 | Smith Kline & French Laboratories Limited | 3,5-Substituted-2-pyridyl-alkylaminocyclobutenediones having histamine h1 -antagonist activity |
IL92011A0 (en) | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
US5534520A (en) | 1990-04-10 | 1996-07-09 | Fisher; Abraham | Spiro compounds containing five-membered rings |
AU2436792A (en) | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
US5629322A (en) | 1994-11-15 | 1997-05-13 | Merck & Co., Inc. | Cyclic amidine analogs as inhibitors of nitric oxide synthase |
WO1999004917A1 (fr) | 1997-07-28 | 1999-02-04 | Ober Utensili Pneumatici S.R.L. | Pistolet a riveter pneumatico-hydraulique |
AU3704400A (en) | 1999-03-04 | 2000-09-21 | E.I. Du Pont De Nemours And Company | Fused bicyclic oxazinone and thiazinone fungicides |
US7161962B1 (en) | 1999-05-27 | 2007-01-09 | Nuera Communications, Inc. | Method and apparatus for coding modem signals for transmission over voice networks |
WO2003014075A2 (fr) | 2001-08-03 | 2003-02-20 | Schering Corporation | Nouveaux inhibiteurs de gamma-secretase |
US6673821B2 (en) | 2001-10-22 | 2004-01-06 | Enanta Pharmaceuticals, Inc. | Nitrogen heterocycle inhibitors of aspartyl protease |
GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
CA2512111A1 (fr) | 2003-01-07 | 2004-07-29 | Merck And Co., Inc. | Inhibiteurs de beta-secretase macrocyclique pour traiter la maladie d'alzheimer |
US7244764B2 (en) | 2003-06-23 | 2007-07-17 | Neurochem (International) Limited | Methods and compositions for treating amyloid-related diseases |
US7291620B2 (en) | 2003-06-30 | 2007-11-06 | Merck + Co., Inc. | N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
EP1643986A4 (fr) | 2003-07-01 | 2009-04-08 | Merck & Co Inc | Inhibiteurs de la beta-secretase de phenylcarboxylate destines au traitement de la maladie d'alzheimer |
EP1660443B1 (fr) * | 2003-08-08 | 2009-03-04 | Schering Corporation | Inhibiteurs bace-1 amines cycliques a substituant benzamide |
TW200524910A (en) | 2003-08-08 | 2005-08-01 | Schering Corp | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
WO2005032471A2 (fr) | 2003-10-03 | 2005-04-14 | Merck & Co., Inc. | Inhibiteurs de type benzylether et benzylamino de beta-secretase pour le traitement de la maladie d'alzheimer |
US20060034848A1 (en) | 2003-11-07 | 2006-02-16 | Ayae Kinoshita | Methods and compositions for treating Alzheimer's disease |
WO2005051914A1 (fr) | 2003-11-24 | 2005-06-09 | Merck & Co., Inc. | Inhibiteurs de benzylether et benzylamino de beta-secretase pour traiter la maladie d'alzheimer |
TW200619203A (en) * | 2003-12-15 | 2006-06-16 | Schering Corp | Heterocyclic aspartyl protease inhibitors |
CN102627609B (zh) * | 2003-12-15 | 2016-05-04 | 默沙东公司 | 杂环天冬氨酰蛋白酶抑制剂 |
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
JP2007517781A (ja) | 2003-12-19 | 2007-07-05 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病治療用のフェニルアミドおよびピリジルアミド系β−セクレターゼ阻害薬 |
CN1942457A (zh) | 2004-04-20 | 2007-04-04 | 默克公司 | 作为β-促分泌酶抑制剂用于阿尔茨海默氏病的治疗中的1,3,5-取代的苯基衍生化合物 |
JP4764418B2 (ja) | 2004-04-20 | 2011-09-07 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な2,4,6−置換ピリジル誘導体化合物 |
EP1740575A2 (fr) | 2004-04-22 | 2007-01-10 | Eli Lilly And Company | Inhibiteurs de la bace |
US7714021B2 (en) | 2004-06-15 | 2010-05-11 | Merck & Co., Inc. | Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease |
CN1968945A (zh) | 2004-06-16 | 2007-05-23 | 惠氏公司 | 用于抑制β分泌酶的氨基-5,5-二苯基咪唑酮衍生物 |
AU2005264917A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of B-secretase |
MX2007000760A (es) | 2004-07-22 | 2007-04-09 | Schering Corp | Amida sustituida inhibidora de b secretasa. |
ES2306200T3 (es) | 2004-07-28 | 2008-11-01 | Schering Corporation | Inhibidores macrociclicos de beta-secretasa. |
CA2583342A1 (fr) | 2004-10-13 | 2006-04-27 | Merck And Co., Inc. | Composes de spiropiperidine utilises comme inhibiteurs de beta-secretase en vue du traitement de la maladie d'alzheimer |
JP2008516946A (ja) | 2004-10-15 | 2008-05-22 | アストラゼネカ・アクチエボラーグ | 置換されたアミノ−ピリミドンおよびそれらの使用 |
WO2006041404A1 (fr) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Composes amino substitues et utilisation de ces compose |
US7932275B2 (en) | 2004-10-29 | 2011-04-26 | Merck, Sharp & Dohme Corp. | 2-aminopyridine compounds useful as β-secretase inhibitors for the treatment of alzheimer's disease |
WO2006057983A1 (fr) | 2004-11-23 | 2006-06-01 | Merck & Co., Inc. | Inhibiteurs de l'aminopyridyle de la beta-secretase macrocyclique permettant de traiter la maladie d'alzheimer |
SG123624A1 (en) * | 2004-12-17 | 2006-07-26 | Singapore Tech Dynamics Pte | An apparatus for altering the course of travellingof a moving article and a method thereof |
BRPI0606690A2 (pt) | 2005-01-14 | 2009-07-14 | Wyeth Corp | composto; uso do composto para o tratamento de uma doença ou distúrbio associado com uma atividade excessiva de bace; e composição farmacêutica |
CN101106994A (zh) | 2005-01-19 | 2008-01-16 | 默克公司 | 用于治疗阿尔茨海默氏病的氨基甲基β-分泌酶抑制剂 |
US8338614B2 (en) | 2005-01-19 | 2012-12-25 | Merck, Sharp & Dohme Corp. | Tertiary carbinamines having substituted heterocycles which are active as β-secretase inhibitors for the treatment of alzheimer's disease |
DE102005023943A1 (de) | 2005-05-20 | 2006-11-23 | Grünenthal GmbH | Pentafluorsulfanyl-substituierte Verbindung und deren Verwendung zur Herstellung von Arzneimitteln |
WO2006138264A2 (fr) | 2005-06-14 | 2006-12-28 | Schering Corporation | Inhibiteurs d'aspartyl protease |
JP2008543846A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | プロテアーゼ阻害剤として化合物の調製およびその使用 |
AU2006259609A1 (en) | 2005-06-14 | 2006-12-28 | Pharmacopeia, Inc. | Aspartyl protease inhibitors |
ATE489370T1 (de) | 2005-06-14 | 2010-12-15 | Schering Corp | Herstellung und verwendung von verbindungen als aspartylproteasehemmer |
AR056865A1 (es) | 2005-06-14 | 2007-10-31 | Schering Corp | Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas |
CA2610812A1 (fr) | 2005-06-14 | 2006-12-28 | Schering Corporation | Inhibiteurs de l'aspartyl protease |
CN101193892A (zh) | 2005-06-14 | 2008-06-04 | 先灵公司 | 大环杂环天冬氨酰基蛋白酶抑制剂 |
TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
AU2006266167A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
WO2007011810A1 (fr) | 2005-07-18 | 2007-01-25 | Merck & Co., Inc. | Inhibiteurs de beta-secretase de spiropiperidine destines au traitement de la maladie d'alzheimer |
TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
US7816378B2 (en) | 2005-08-03 | 2010-10-19 | Merck Sharp & Dohme Corp. | Cyclic ketal beta-secretase inhibitors for the treatment of alzheimer's disease |
US20090170830A1 (en) | 2005-08-03 | 2009-07-02 | Nantermet Philippe G | Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease |
CA2623245A1 (fr) | 2005-09-26 | 2007-04-05 | Wyeth | Composes d'amino-5-[4-(difluoromethoxy) phenyl]-5-phenylimidazolone utilises comme inhibiteurs de la beta-secretase (bace) |
CN103936690B (zh) | 2005-10-25 | 2016-06-08 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
WO2007050721A2 (fr) | 2005-10-27 | 2007-05-03 | Schering Corporation | Inhibiteurs heterocycliques d'aspartyle protease |
EP1943246A1 (fr) | 2005-10-31 | 2008-07-16 | Schering Corporation | Inhibiteurs de l aspartyle protease |
EP1951680A4 (fr) | 2005-11-15 | 2011-08-10 | Astrazeneca Ab | Nouveaux derives de 2-aminopyrimidinone et leur utilisation |
TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
CN101360722A (zh) | 2005-11-15 | 2009-02-04 | 阿斯利康(瑞典)有限公司 | 新颖的2-氨基嘧啶衍生物及其用途 |
CA2629317A1 (fr) | 2005-11-16 | 2007-05-24 | Merck & Co., Inc. | Composes d'imidazolidinone utiles en tant qu'inhibiteurs de la beta-secretase lors du traitement de la maladie d'alzheimer |
EP1954682A4 (fr) | 2005-11-21 | 2011-11-09 | Astrazeneca Ab | Nouveaux composes 2-amino-imidazole-4-one et leur utilisation dans la fabrication d'un medicament destine a etre utilise dans le traitement d'une deficience cognitive, la maladie d'alzheimer, le neurodegenerescence et la demence |
TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
EP1966185A2 (fr) | 2005-12-19 | 2008-09-10 | Wyeth a Corporation of the State of Delaware | DÉRIVÉS DE 2-AMINO-5-PIPÉRIDINYLIMIDAZOLONE ET APPLICATIONS À LA MODULATION DE LA ß-SECRÉTASE |
GB0602951D0 (en) | 2006-02-14 | 2006-03-29 | Novartis Ag | Organic Compounds |
WO2007100536A1 (fr) | 2006-02-24 | 2007-09-07 | Wyeth | COMPOSES DE DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] POUR L'INHIBITION DE LA β-SECRETASE |
EP2004630A4 (fr) | 2006-04-05 | 2010-05-19 | Astrazeneca Ab | 2-aminopyrimidin-4-ones et leur utilisation pour le traitement ou la prevention de pathologies liees a la proteine a |
EP2032542A2 (fr) | 2006-06-12 | 2009-03-11 | Schering Corporation | Inhibiteurs d'aspartyl protéase hétérocycliques |
TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
TW200817406A (en) | 2006-08-17 | 2008-04-16 | Wyeth Corp | Imidazole amines as inhibitors of β-secretase |
AU2007293416A1 (en) | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease |
EP2077719B1 (fr) | 2006-09-21 | 2011-12-28 | Merck Sharp & Dohme Corp. | Inhibiteurs pipéridines et pyrrolidines de la bêta-secrétase utilisés dans le traitement de la maladie d'alzheimer |
JP2010505833A (ja) | 2006-10-06 | 2010-02-25 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病を治療するためのマクロ環式スピロピペリジンβ−セクレターゼ阻害剤 |
CA2668065A1 (fr) | 2006-10-30 | 2008-05-08 | Merck & Co., Inc. | Composes de spiropiperidine inhibiteurs de la beta-secretase pour le traitement de la maladie d'alzheimer |
WO2008063114A1 (fr) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino-imidazolones et utilisation thérapeutique de ces composés pour traiter les troubles cognitifs, la maladie d'alzheimer, la neurodégénérescence et la démence |
CN101631779A (zh) | 2006-12-12 | 2010-01-20 | 先灵公司 | 含有三环系统的天冬氨酰蛋白酶抑制剂 |
AU2007332754A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
WO2008076044A1 (fr) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Nouveaux 2-amino-5, 5-diaryl-imidazol-4-ones |
TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
PE20090160A1 (es) | 2007-03-20 | 2009-02-11 | Wyeth Corp | COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA |
AR065814A1 (es) | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
JP5383483B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
EP2147914B1 (fr) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Dérivés d'aminodihydrothiazine substitués par des groupes cycliques |
WO2009015917A2 (fr) | 2007-05-14 | 2009-02-05 | F. Hoffmann-La Roche Ag | Inhibiteurs dihydroquinone et dihydronaphtridine de jnk |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
WO2009005470A1 (fr) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Dérivés d'isoindole substitués aryle et hétéroaryle en tant qu'inhibiteurs de la bace |
WO2009005471A1 (fr) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Dérivés d'isoindole substitués aryle et hétéroaryle en tant qu'inhibiteurs de la bace |
PE20090957A1 (es) | 2007-08-06 | 2009-07-13 | Schering Corp | Moduladores de gamma secretasa |
US20090041201A1 (en) | 2007-08-06 | 2009-02-12 | Carestream Health, Inc. | Alignment apparatus for imaging system |
RU2476431C2 (ru) | 2008-01-18 | 2013-02-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Конденсированное производное аминодигидротиазина |
MX2010008347A (es) | 2008-02-18 | 2010-11-12 | Hoffmann La Roche | Derivados de 4,5-dihidro-oxazol-2-ilamina. |
JP2011514342A (ja) | 2008-02-28 | 2011-05-06 | メルク・シャープ・エンド・ドーム・コーポレイション | アルツハイマー病治療用2−アミノイミダゾールベータ−セクレターゼ阻害剤 |
AR071385A1 (es) * | 2008-04-22 | 2010-06-16 | Schering Corp | Compuestos de 2-imino-3-metil pirrolopirimidinona sustituida con tiofenilo,composiciones farmaceuticas que los contienen,y uso de los mismos para el tratamiento de patologias asociadas con la proteina beta amiloide,tales como alzheimer y otros formas de demencia. |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
EA201001566A1 (ru) | 2008-05-05 | 2011-04-29 | Пфайзер Инк. | Новый класс спиропиперидинов для лечения нейродегенеративных заболеваний |
ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
WO2010013302A1 (fr) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Dérivé de spiroaminodihydrothiazine |
WO2010013794A1 (fr) | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Dérivés de spiroaminodihydrothiazine |
US8450308B2 (en) | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
WO2010030954A1 (fr) | 2008-09-11 | 2010-03-18 | Amgen Inc. | Composés cycliques spiro-tétracycliques utiles en tant que modulateurs de la bêta-sécrétase et leurs procédés d'utilisation |
AR073406A1 (es) | 2008-09-30 | 2010-11-03 | Eisai R&D Man Co Ltd | Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer. |
WO2010048149A2 (fr) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Modulateurs hétérocycliques de gpr119 pour le traitement d'une maladie |
JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
US20100125087A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
US20100125081A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
WO2010063718A1 (fr) | 2008-12-02 | 2010-06-10 | ETH Zürich | Essai de criblage pour des agents thérapeutiques contre une maladie métabolique |
EP2398789B1 (fr) | 2009-02-20 | 2014-03-19 | Merck Sharp & Dohme Corp. | Inhibiteurs de bêta-sécrétase de type spiropyrrolidine pour le traitement de la maladie d'alzheimer |
TWI464153B (zh) | 2009-03-13 | 2014-12-11 | Vitae Pharmaceuticals Inc | β-分泌酶之抑制劑 |
WO2010113848A1 (fr) | 2009-03-31 | 2010-10-07 | 塩野義製薬株式会社 | Dérivé isothiourée ou dérivé isourée ayant une activité inhibitrice de bace1 |
US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
TW201105650A (en) | 2009-07-02 | 2011-02-16 | Astrazeneca Ab | New compounds |
WO2011002409A1 (fr) | 2009-07-02 | 2011-01-06 | Astrazeneca Ab | Inhibiteurs de bêta-secrétase dérivés de 5h-pyrrolo[3,4-b>]pyrazine-7-amine |
AR077365A1 (es) | 2009-07-02 | 2011-08-24 | Astrazeneca Ab | Derivados de imidazol para el tratamiento de enfermedades mediadas por la inhibicion de la formacion de abeta |
AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
UY32799A (es) | 2009-07-24 | 2011-02-28 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos |
US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
EP2485591B1 (fr) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Composés de type dioxyde d'imino-thiadiazine utilisés en tant qu'inhibiteurs de bace, compositions en contenant et leur utilisation |
UA108363C2 (uk) * | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
EP2485590B1 (fr) * | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Composés hétérocycliques de type imino-pentafluorosulfure utilisés en tant qu'inhibiteurs de bace1, compositions en contenant et leur utilisation |
JPWO2011058763A1 (ja) | 2009-11-13 | 2013-03-28 | 塩野義製薬株式会社 | アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体 |
WO2011072064A1 (fr) | 2009-12-08 | 2011-06-16 | Array Biopharma Inc. | Spiro[chromane-4,4'-imidazol]ones en tant qu'inhibiteurs de bêta-sécrétase |
WO2011071057A1 (fr) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | Composition pharmaceutique pour le traitement ou la prévention de la maladie d'alzheimer contenant un dérivé hétérocyclique contenant du soufre |
US20120245154A1 (en) | 2009-12-09 | 2012-09-27 | Shionogi & Co., Ltd. | Substituted aminothiazine derivative |
US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
EP2511269A4 (fr) | 2009-12-11 | 2013-04-24 | Shionogi & Co | Composé hétérocyclique fusionné comportant un groupement amino |
US20120258961A1 (en) | 2009-12-24 | 2012-10-11 | Shionogi & Co., Ltd. | 4-amino-1,3-thiazine or oxazine derivative |
US20120277244A1 (en) | 2009-12-31 | 2012-11-01 | Novartis Ag | Pyrazine derivatives and their use in the treatment of neurological disorders |
CA2788363A1 (fr) | 2010-01-19 | 2011-07-28 | Amgen Inc. | Composes d'aminoheteroaryle en tant que modulateurs de beta-secretase et procedes d'utilisation |
CN102812005B (zh) | 2010-02-24 | 2014-12-10 | 生命医药公司 | β-分泌酶抑制剂 |
JP2013522305A (ja) | 2010-03-15 | 2013-06-13 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのスピロ−四環式環化合物 |
ES2450568T3 (es) | 2010-03-15 | 2014-03-25 | Amgen Inc. | Compuestos espiero de amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso médico |
US20120065195A1 (en) | 2010-03-31 | 2012-03-15 | Clark Christopher T | Compounds for treating neurodegenerative diseases |
US20130108645A1 (en) | 2010-04-13 | 2013-05-02 | The Johns Hopkins University | Methods for enhancing axonal regeneration |
WO2011130741A1 (fr) | 2010-04-16 | 2011-10-20 | Array Biopharma Inc. | Composés pour le traitement de maladies neurodégénératives |
US8673894B2 (en) | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
TW201144295A (en) | 2010-05-12 | 2011-12-16 | Astrazeneca Ab | Hemifumarate salt |
SG185652A1 (en) | 2010-06-09 | 2012-12-28 | Janssen Pharmaceutica Nv | 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) |
TWI537263B (zh) | 2010-06-09 | 2016-06-11 | 健生藥品公司 | 使用作為β-分泌酶抑制劑之5,6-二氫-2H-[1,4]-3-基-胺衍生物 |
KR101265451B1 (ko) | 2010-07-13 | 2013-05-22 | 노파르티스 아게 | 옥사진 유도체, 및 신경계 장애의 치료에 있어서의 그의 용도 |
US8815881B2 (en) | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
US20120083501A1 (en) | 2010-09-24 | 2012-04-05 | Hunt Kevin W | Compounds for treating neurodegenerative diseases |
JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
US8927721B2 (en) | 2010-10-29 | 2015-01-06 | Shionogi & Co., Ltd. | Naphthyridine derivative |
AR083953A1 (es) | 2010-11-22 | 2013-04-10 | Array Biopharma Inc | Compuestos para tratar enfermedades neurodegenerativas |
EP2643325A1 (fr) | 2010-11-23 | 2013-10-02 | Amgen Inc. | Spiro-amino-imidazolones et spiro-amino-dihydro-pyrimidinones en tant que modulateurs de bêta-sécrétase et leurs méthodes d'utilisation |
US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
US8399459B2 (en) | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
US8404680B2 (en) | 2011-02-08 | 2013-03-26 | Hoffmann-La Roche Inc. | N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors |
US9145426B2 (en) * | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
JP2012250933A (ja) | 2011-06-03 | 2012-12-20 | Shionogi & Co Ltd | オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物 |
US9181236B2 (en) * | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
-
2010
- 2010-06-10 UA UAA201205617A patent/UA108363C2/ru unknown
- 2010-10-06 EP EP10822567.3A patent/EP2485736B1/fr active Active
- 2010-10-06 NZ NZ598694A patent/NZ598694A/en unknown
- 2010-10-06 HU HUE10822567A patent/HUE028672T2/en unknown
- 2010-10-06 JP JP2012533260A patent/JP5592494B2/ja active Active
- 2010-10-06 WO PCT/US2010/051553 patent/WO2011044181A1/fr active Application Filing
- 2010-10-06 PL PL10822567T patent/PL2485736T3/pl unknown
- 2010-10-06 MY MYPI2012001495A patent/MY163744A/en unknown
- 2010-10-06 KR KR1020147005914A patent/KR101646424B1/ko active IP Right Grant
- 2010-10-06 PE PE2012000800A patent/PE20141935A1/es active IP Right Grant
- 2010-10-06 KR KR1020127011742A patent/KR101435301B1/ko active IP Right Grant
- 2010-10-06 ME MEP-2016-36A patent/ME02366B/fr unknown
- 2010-10-06 SG SG10201406365WA patent/SG10201406365WA/en unknown
- 2010-10-06 RS RS20160099A patent/RS54587B1/en unknown
- 2010-10-06 AU AU2010303591A patent/AU2010303591B2/en active Active
- 2010-10-06 ES ES15197990T patent/ES2773908T3/es active Active
- 2010-10-06 PT PT108225673T patent/PT2485736E/pt unknown
- 2010-10-06 KR KR1020167020935A patent/KR101759856B1/ko active IP Right Grant
- 2010-10-06 CN CN201510085341.8A patent/CN104744403A/zh active Pending
- 2010-10-06 EA EA201270505A patent/EA025120B1/ru not_active IP Right Cessation
- 2010-10-06 DK DK10822567.3T patent/DK2485736T3/en active
- 2010-10-06 GE GEAP201012693A patent/GEP20156366B/en unknown
- 2010-10-06 CN CN201080055589.5A patent/CN102639135B/zh active Active
- 2010-10-06 SI SI201031126T patent/SI2485736T1/sl unknown
- 2010-10-06 CA CA2774579A patent/CA2774579C/fr active Active
- 2010-10-06 TW TW100118230A patent/TWI477502B/zh active
- 2010-10-06 TW TW104103783A patent/TW201520192A/zh unknown
- 2010-10-06 AR ARP100103627 patent/AR078534A1/es active IP Right Grant
- 2010-10-06 US US13/392,297 patent/US8729071B2/en active Active
- 2010-10-06 TW TW099134074A patent/TWI477501B/zh active
- 2010-10-06 MX MX2012004148A patent/MX2012004148A/es active IP Right Grant
- 2010-10-06 BR BR112012008014-8A patent/BR112012008014B1/pt active IP Right Grant
- 2010-10-06 EP EP15197990.3A patent/EP3034080B1/fr active Active
- 2010-10-06 ES ES10822567.3T patent/ES2560788T3/es active Active
-
2012
- 2012-03-12 TN TNP2012000112A patent/TN2012000112A1/en unknown
- 2012-03-15 DO DO2012000067A patent/DOP2012000067A/es unknown
- 2012-03-18 IL IL218712A patent/IL218712A/en active IP Right Grant
- 2012-03-20 NI NI201200044A patent/NI201200044A/es unknown
- 2012-03-29 CR CR20120158A patent/CR20120158A/es unknown
- 2012-03-29 HN HN2012000612A patent/HN2012000612A/es unknown
- 2012-04-04 CL CL2012000872A patent/CL2012000872A1/es unknown
- 2012-04-05 ZA ZA201202517A patent/ZA201202517B/en unknown
- 2012-04-27 EC ECSP12011857 patent/ECSP12011857A/es unknown
- 2012-05-04 MA MA34836A patent/MA33726B1/fr unknown
- 2012-08-27 HK HK12108359.4A patent/HK1167608A1/xx unknown
-
2014
- 2014-02-11 IL IL230926A patent/IL230926A/en active IP Right Grant
- 2014-03-21 US US14/221,650 patent/US9428475B2/en active Active
- 2014-03-21 US US14/221,644 patent/US8940748B2/en active Active
- 2014-03-21 US US14/221,640 patent/US9029362B2/en active Active
- 2014-05-09 JP JP2014097694A patent/JP6023749B2/ja active Active
- 2014-07-31 JP JP2014155749A patent/JP5976733B2/ja active Active
-
2015
- 2015-02-27 US US14/633,952 patent/US9475785B2/en active Active
- 2015-07-08 IL IL239833A patent/IL239833A0/en unknown
-
2016
- 2016-02-22 HR HRP20160185T patent/HRP20160185T1/hr unknown
- 2016-06-27 HK HK16107439.6A patent/HK1219419A1/zh unknown
- 2016-06-29 JP JP2016128750A patent/JP2017002052A/ja not_active Withdrawn
- 2016-08-29 US US15/250,338 patent/US9687494B2/en active Active
- 2016-12-21 ZA ZA2016/08799A patent/ZA201608799B/en unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
MA33726B1 (fr) | Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation | |
MA47447B1 (fr) | 2-hétéroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides pour le traitement du cancer | |
MA31283B1 (fr) | Produits dérivés de 2,3-dihydroimidazo[1,2-c]quinazoline substitués, utiles pour le traitement de troubles hyperlifératifs et de maladies associées à une angiogénèse | |
MA32070B1 (fr) | Dérivés hétérocycliques réunis par fusion et procédés d'utilisation associés | |
TN2009000471A1 (fr) | Composes amino-heterocycliques | |
MA30406B1 (fr) | Nouveaux composes | |
MA28437B1 (fr) | Composes et leurs procedes d'utilisation | |
MA35285B1 (fr) | Indazoles | |
MA35422B1 (fr) | Imidazopyridazines amino-substituees | |
MA44674B1 (fr) | Inhibiteurs de bromodomaine | |
MA33239B1 (fr) | 3h-imidazo [4,5-c] pyridine-6-carboxamides en tant qu'anti-inflammatoires | |
MA33450B1 (fr) | Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques | |
MA30333B1 (fr) | Aminotetrahydropyranes utiles en tant qu'inhibiteurs de la dipeptidyle peptidase-iv pour le traitement ou la prevention du diabete. | |
MA34898B1 (fr) | Nouveaux dérivés hétérocycliques et leur utilisation dans le traitement de troubles neurologiques | |
MA35114B1 (fr) | 1,3-oxazines à titre d'inhibiteurs de bace1 et/ou de bace2 | |
TNSN08445A1 (fr) | Derives de triazolopyrazine utiles comme agent anticancereux | |
TNSN07476A1 (fr) | Derives de n-(pyridine -2- yl) - sulfonamide | |
MA30163B1 (fr) | Anticorps monoclonaux specifiques pour a beta 1-42 ayant des proprietes therapeutiques | |
MA33467B1 (fr) | Promédicaments comprenant un conjugué insuline-lieur | |
MA33295B1 (fr) | Nouvelle formulation de diclofénac | |
MA29411B1 (fr) | 1h-quinazoline -2,4-diones et leur utilisation en tant que ligands du recepteur ampa | |
MA33178B1 (fr) | Pipéridines substituées comme antagonistes de ccr3 | |
MA29685B1 (fr) | Composes spiroheterocycliques et leurs utilisations en tant qu'agents therapeutiques | |
MA30514B1 (fr) | Nouveaux composes. | |
MA54653B1 (fr) | Modulateurs du récepteur de cxcr7 pipéridine |