AR100810A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents
Inhibidores de fosfatidilinositol 3-quinasaInfo
- Publication number
- AR100810A1 AR100810A1 ARP150101860A ARP150101860A AR100810A1 AR 100810 A1 AR100810 A1 AR 100810A1 AR P150101860 A ARP150101860 A AR P150101860A AR P150101860 A ARP150101860 A AR P150101860A AR 100810 A1 AR100810 A1 AR 100810A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- carbon atoms
- substituted carbon
- alkyl
- halo
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 15
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 102000038030 PI3Ks Human genes 0.000 abstract 4
- 108091007960 PI3Ks Proteins 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 2
- 102000001708 Protein Isoforms Human genes 0.000 abstract 2
- 108010029485 Protein Isoforms Proteins 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
-
- 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
- C07D403/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P31/12—Antivirals
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
Abstract
Los compuestos son inhibidores de las actividades de la fosfatidilinositol 3-quinasa (Pl3K) y son útiles para el tratamiento de condiciones mediadas por una o más isoformas de PI3K. La presente solicitud provee adicionalmente composiciones farmacéuticas que incluyen un compuesto de fórmula (1), o sales, isómeros, tautómeros o mezclas de los mismos farmacéuticamente aceptables, y métodos para utilizar estos compuestos y composiciones para el tratamiento de condiciones mediadas por una o más isoformas de PI3K. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) en donde: n es 1, 2, ó 3; m es 0 ó 1; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono sustituido opcionalmente, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alcoxi de uno a seis átomos de carbono sustituido opcionalmente, sulfonilo sustituido opcionalmente, arilo de tres a ocho átomos de carbono sustituido opcionalmente, heteroarilo de tres a ocho átomos de carbono sustituido opcionalmente, cicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente, y heterocicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente; cada R² es independientemente de halo y alquilo de uno a seis átomos de carbono sustituido opcionalmente; R³ es hidrógeno, alquilo de uno a seis átomos de carbono sustituido opcionalmente, arilo de seis a diez átomos de carbono opcionalmente sustituido, o cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos un grupo aromático y al menos dos heteroátomos seleccionados de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionados independientemente de halo, ciano, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alquilo de uno a seis átomos de carbono sustituido opcionalmente, alquinilo de dos a cuatro átomos de carbono sustituido opcionalmente, y -NH₂; y R⁵ es hidrógeno o alquilo de uno a seis átomos de carbono sustituido opcionalmente, en donde R⁵ y R³ junto con los átomos a los cuales están enlazados forman un anillo heterocíclico de cuatro a ocho miembros; o una sal, isómero, o una mezcla de los mismos, farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462011905P | 2014-06-13 | 2014-06-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR100810A1 true AR100810A1 (es) | 2016-11-02 |
Family
ID=54545432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150101860A AR100810A1 (es) | 2014-06-13 | 2015-06-11 | Inhibidores de fosfatidilinositol 3-quinasa |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9499523B2 (es) |
| EP (1) | EP3154962B1 (es) |
| JP (1) | JP6346964B2 (es) |
| KR (1) | KR20170012558A (es) |
| CN (1) | CN106573922A (es) |
| AR (1) | AR100810A1 (es) |
| AU (1) | AU2015274637B2 (es) |
| BR (1) | BR112016028814A2 (es) |
| CA (1) | CA2952044C (es) |
| EA (1) | EA201692265A1 (es) |
| ES (1) | ES2750357T3 (es) |
| IL (1) | IL249079A0 (es) |
| MX (1) | MX2016016517A (es) |
| NZ (1) | NZ726638A (es) |
| SG (1) | SG11201610088XA (es) |
| TW (1) | TW201627303A (es) |
| WO (1) | WO2015191754A2 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2763103T3 (es) | 2014-06-13 | 2020-05-27 | Gilead Sciences Inc | Inhibidor de la fosfatidilinositol 3-quinasa |
| JP6454736B2 (ja) | 2014-06-13 | 2019-01-16 | ギリアード サイエンシーズ, インコーポレイテッド | ホスファチジルイノシトール3−キナーゼ阻害剤 |
| CN106459005A (zh) | 2014-06-13 | 2017-02-22 | 吉利德科学公司 | 磷脂酰肌醇3‑激酶抑制剂 |
| WO2015191754A2 (en) | 2014-06-13 | 2015-12-17 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| BR112016028876A2 (pt) | 2014-06-13 | 2017-08-22 | Gilead Sciences Inc | composto, composição farmacêutica, método para tratar uma doença ou condição em um ser humano, kit, e, uso de um composto, um sal, isômero ou uma mistura farmaceuticamente aceitável dos mesmos. |
| SG11201705069YA (en) | 2014-12-26 | 2017-07-28 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| 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 |
| 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 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) * | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| PL3706762T3 (pl) | 2017-12-07 | 2025-02-10 | Emory University | N4-hydroksycytydyna i pochodne oraz związane z nimi zastosowania przeciwwirusowe |
| WO2019143874A1 (en) | 2018-01-20 | 2019-07-25 | Sunshine Lake Pharma Co., Ltd. | Substituted aminopyrimidine compounds and methods of use |
| MX2022007930A (es) * | 2019-12-24 | 2022-08-08 | Carna Biosciences Inc | Compuestos moduladores de diacilglicerol quinasa. |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US5182297A (en) | 1988-02-25 | 1993-01-26 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5059714A (en) | 1988-02-25 | 1991-10-22 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4943593A (en) | 1988-02-25 | 1990-07-24 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4965288A (en) | 1988-02-25 | 1990-10-23 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5252608A (en) | 1988-02-25 | 1993-10-12 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5021456A (en) | 1988-02-25 | 1991-06-04 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| US5120764A (en) | 1988-11-01 | 1992-06-09 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US4997854A (en) | 1989-08-25 | 1991-03-05 | Trustees Of Boston University | Anti-fibrotic agents and methods for inhibiting the activity of lysyl oxidase in-situ using adjacently positioned diamine analogue substrates |
| KR100785363B1 (ko) | 2000-04-25 | 2007-12-18 | 이코스 코포레이션 | 인간 포스파티딜-이노시톨 3-키나제 델타의 억제제 |
| US6667300B2 (en) * | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| FR2828206B1 (fr) | 2001-08-03 | 2004-09-24 | Centre Nat Rech Scient | Utilisation d'inhibiteurs des lysyl oxydases pour la culture cellulaire et le genie tissulaire |
| HUE029188T2 (en) | 2007-03-12 | 2017-03-28 | Ym Biosciences Australia Pty | Phenylamino-pyrimidine compounds and their use |
| US8450321B2 (en) | 2008-12-08 | 2013-05-28 | Gilead Connecticut, Inc. | 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor |
| US8399460B2 (en) | 2009-10-27 | 2013-03-19 | Astrazeneca Ab | Chromenone derivatives |
| CA2785499C (en) * | 2009-12-22 | 2017-05-02 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| AU2011260961B9 (en) | 2010-05-31 | 2015-02-26 | Ono Pharmaceutical Co., Ltd. | Purinone derivative |
| AU2011302196B2 (en) * | 2010-09-14 | 2016-04-28 | Exelixis, Inc. | Inhibitors of PI3K-delta and methods of their use and manufacture |
| PE20140192A1 (es) | 2010-10-06 | 2014-02-24 | Glaxosmithkline Llc | Derivados de bencimidazol como inhibidores de cinasa pi3 |
| WO2012089633A1 (fr) | 2010-12-28 | 2012-07-05 | Sanofi | Nouveaux derives de pyrimidines, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb) |
| EP2518070A1 (en) * | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Pyrrolotriazinone derivatives as PI3K inhibitors |
| ES2763103T3 (es) | 2014-06-13 | 2020-05-27 | Gilead Sciences Inc | Inhibidor de la fosfatidilinositol 3-quinasa |
| CN106459005A (zh) | 2014-06-13 | 2017-02-22 | 吉利德科学公司 | 磷脂酰肌醇3‑激酶抑制剂 |
| JP6454736B2 (ja) | 2014-06-13 | 2019-01-16 | ギリアード サイエンシーズ, インコーポレイテッド | ホスファチジルイノシトール3−キナーゼ阻害剤 |
| WO2015191754A2 (en) | 2014-06-13 | 2015-12-17 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| BR112016028876A2 (pt) | 2014-06-13 | 2017-08-22 | Gilead Sciences Inc | composto, composição farmacêutica, método para tratar uma doença ou condição em um ser humano, kit, e, uso de um composto, um sal, isômero ou uma mistura farmaceuticamente aceitável dos mesmos. |
-
2015
- 2015-06-10 WO PCT/US2015/035161 patent/WO2015191754A2/en not_active Ceased
- 2015-06-10 KR KR1020177000693A patent/KR20170012558A/ko not_active Ceased
- 2015-06-10 BR BR112016028814A patent/BR112016028814A2/pt not_active IP Right Cessation
- 2015-06-10 SG SG11201610088XA patent/SG11201610088XA/en unknown
- 2015-06-10 EP EP15795017.1A patent/EP3154962B1/en active Active
- 2015-06-10 MX MX2016016517A patent/MX2016016517A/es unknown
- 2015-06-10 CA CA2952044A patent/CA2952044C/en not_active Expired - Fee Related
- 2015-06-10 CN CN201580031602.6A patent/CN106573922A/zh active Pending
- 2015-06-10 US US14/736,025 patent/US9499523B2/en active Active
- 2015-06-10 ES ES15795017T patent/ES2750357T3/es active Active
- 2015-06-10 AU AU2015274637A patent/AU2015274637B2/en not_active Ceased
- 2015-06-10 NZ NZ726638A patent/NZ726638A/en not_active IP Right Cessation
- 2015-06-10 JP JP2016572435A patent/JP6346964B2/ja not_active Expired - Fee Related
- 2015-06-10 EA EA201692265A patent/EA201692265A1/ru unknown
- 2015-06-11 AR ARP150101860A patent/AR100810A1/es unknown
- 2015-06-12 TW TW104119194A patent/TW201627303A/zh unknown
-
2016
- 2016-11-21 IL IL249079A patent/IL249079A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20170012558A (ko) | 2017-02-02 |
| IL249079A0 (en) | 2017-01-31 |
| ES2750357T3 (es) | 2020-03-25 |
| MX2016016517A (es) | 2017-05-01 |
| AU2015274637B2 (en) | 2018-04-19 |
| TW201627303A (zh) | 2016-08-01 |
| CA2952044C (en) | 2019-01-29 |
| AU2015274637A1 (en) | 2016-12-08 |
| SG11201610088XA (en) | 2016-12-29 |
| CN106573922A (zh) | 2017-04-19 |
| JP2017517544A (ja) | 2017-06-29 |
| EP3154962B1 (en) | 2019-08-07 |
| WO2015191754A2 (en) | 2015-12-17 |
| CA2952044A1 (en) | 2015-12-17 |
| EP3154962A2 (en) | 2017-04-19 |
| US20150361071A1 (en) | 2015-12-17 |
| WO2015191754A3 (en) | 2016-02-11 |
| BR112016028814A2 (pt) | 2017-08-22 |
| NZ726638A (en) | 2018-04-27 |
| EA201692265A1 (ru) | 2017-05-31 |
| US9499523B2 (en) | 2016-11-22 |
| JP6346964B2 (ja) | 2018-06-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR100810A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR100806A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR100809A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR119651A1 (es) | Compuestos heterocíclicos y de heteroarilo para tratar la enfermedad de huntington | |
| AR127309A2 (es) | Derivados de piridazinona | |
| AR100808A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR094313A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR101600A1 (es) | COMPUESTOS DE SPIRO[3H-INDOL-3,2-PIRROLIDIN]-2(1H)-ONA Y DERIVADOS COMO INHIBIDORES DE MDM2-p53 | |
| AR103574A1 (es) | Compuestos tricíclicos y usos de lo mismos en medicina | |
| AR097431A1 (es) | Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim | |
| PE20190656A1 (es) | Compuestos de tiazolo-piridina sustituida como inhibidores de malt1 | |
| AR100438A1 (es) | Pirazolopiridinas y pirazolopirimidinas | |
| AR088029A1 (es) | Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central | |
| AR087591A1 (es) | Derivados de ciclohexil azetidina como inhibidores de jak | |
| AR100886A1 (es) | 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas | |
| AR094314A1 (es) | Inhibidores de fosfatidilinositol 3-cinasa | |
| AR084553A1 (es) | DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER | |
| AR089143A1 (es) | Triazolopiridinas sustituidas con actividad inhibidora de ttk | |
| AR089776A1 (es) | 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir | |
| AR100807A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| PE20142081A1 (es) | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos | |
| AR096846A1 (es) | Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet | |
| AR094550A1 (es) | Inhibidores de btk | |
| AR103742A1 (es) | Derivados de trifluorometilpropanamida | |
| AR085088A1 (es) | Inhibidores de histona desacetilasa y composiciones farmaceuticas que los contienen |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |