AR079840A2 - Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos - Google Patents
Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanosInfo
- Publication number
- AR079840A2 AR079840A2 ARP110100026A ARP110100026A AR079840A2 AR 079840 A2 AR079840 A2 AR 079840A2 AR P110100026 A ARP110100026 A AR P110100026A AR P110100026 A ARP110100026 A AR P110100026A AR 079840 A2 AR079840 A2 AR 079840A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- aryl
- heteroaryl
- compounds
- Prior art date
Links
- -1 amide compounds Chemical class 0.000 abstract 13
- 150000001875 compounds Chemical class 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 230000000694 effects Effects 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 210000003169 central nervous system Anatomy 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000005843 halogen group Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000006721 (C5-C10) heteroaryl (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 abstract 1
- 125000004505 1,2,4-oxadiazol-5-yl group Chemical group O1N=CN=C1* 0.000 abstract 1
- 125000004515 1,2,4-thiadiazol-3-yl group Chemical group S1N=C(N=C1)* 0.000 abstract 1
- 125000004516 1,2,4-thiadiazol-5-yl group Chemical group S1N=CN=C1* 0.000 abstract 1
- 125000004509 1,3,4-oxadiazol-2-yl group Chemical group O1C(=NN=C1)* 0.000 abstract 1
- 125000004521 1,3,4-thiadiazol-2-yl group Chemical group S1C(=NN=C1)* 0.000 abstract 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical group [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 abstract 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 abstract 1
- 125000005330 8 membered heterocyclic group Chemical group 0.000 abstract 1
- 108010009685 Cholinergic Receptors Proteins 0.000 abstract 1
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 abstract 1
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 abstract 1
- 102000034337 acetylcholine receptors Human genes 0.000 abstract 1
- 230000002411 adverse Effects 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 230000036772 blood pressure Effects 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- 230000001537 neural effect Effects 0.000 abstract 1
- 230000000324 neuroprotective effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
- 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
- C07D471/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se revelan compuestos, composiciones farmacéuticas que incluyen los compuestos y métodos de preparacion y el uso de los mismos. Los compuestos son compuestos amida que pueden prepararse desde ciertos ácidos carboxílicos heteroarilos y ciertos diazabicicloalcanos. Los compuestos exhiben selectividad para los receptores nicotínicos neuronales del subtipo alfa4beta2 en el sistema nervioso central (SNC) y se unen con alta afinidad. Los compuestos y composiciones pueden ser utilizados para tratar y/o prevenir una gran variedad de males y enfermedades, particularmente del Sistema Nervioso Central. Los compuestos pueden: (i) alterar el numero de receptores colinérgicos nicotínicos del cerebro del paciente, (ii) exhibir efectos neuroprotectores, y (iii) cuando se utilizan en cantidades efectivas, no dan como resultado efectos colaterales adversos (por ejemplo, efectos colaterales como presion sanguínea y frecuencia cardiaca, efectos negativos importantes en el tracto gastrointestinal y efectos importantes en el musculo oseo). Reivindicacion 1: Un compuesto representado por formula (1) caracterizado porque n tiene el valor de 0 o 1, y Cy es un grupo heteroarilo elegido del grupo de 2-furanilo, 3-furanilo, 2-oxazolilo, 4-oxazolilo, 5-oxazolilo, 3-isoxazolilo, 4-isoxazolilo, 5-isoxazolilo, 1,3,4-oxadiazol-2-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,4-oxadiazol-5-ilo, 2-tiazolilo, 4-tiazolilo, 5-tiazolilo, 3-isotiazolilo, 4-isotiazolilo, 5-isotiazolilo, 1,3,4-tiadiazol-2-ilo, 1,2,4-tiadiazol-3-ilo, 1,2,4-tiadiazol-5-ilo y 4-piridinilo, cuyos grupos heteroarilo son sustituidos opcionalmente con hasta tres sustituyentes no hidrogeno independientemente seleccionados de alquilo C1-6, alquilo C1-6 sustituido, alquenilo C2-6, alquenilo C2-6 sustituido, alquinilo C2-6, alquinilo C2-6 sustituido, heterociclilo de 3 a 8 miembros, heterociclilo de 3 a 8 miembros sustituido, cicloalquilo C3-8, cicloalquilo C3-8 sustituido, arilo C5-10, heteroarilo de 5 a 10 miembros, arilo C5-10 sustituido, heteroarilo de 5 a 10 miembros sustituido, alquilo C1-6-arilo C5-10, alquil C1-6-heteroarilo de 5 a 10 miembros, alquilo C1-6-arilo C5-10 sustituido, alquilo C1-6-heteroarilo de 5 a 10 miembros sustituido, arilo C5-10-alquilo C1-6, heteroarilo de 5 a 10 miembros-alquilo C1-6, arilo C5-10-alquilo C1-6 sustituido, heteroarilo de 5 a 10 miembros-alquilo C1-6 sustituido, halo, -OR', -NR'Rö, -CF3, -CN, -NO2, -C2R', -SR', -N3, -C(=O)NR'Rö, -NR'C(=O)Rö, -C(=O)R', -C(=O)OR', -OC(=O)R', -OC(=O)NR'Rö, -NR'C(=O)ORö, -SO2R', -SO2NR'Rö, y -NR'SO2Rö, donde R' y Rö se seleccionan independientemente del hidrogeno, alquilo C1-6, cicloalquilo C3-8, heterociclilo de 3 a 8 miembros, arilo C5-10, heteroarilo de 5 a 10 miembros y arilo C5-10-alquilo C1-6, o R' y Rö junto con los átomos a los cuales se unen pueden formar un anillo heterocíclico de 3 a 8 miembros, en donde el término ôsustituidoö aplicado a alquilo, alquenilo, alquinilo, heterociclilo, cicloalquilo, arilo, heteroarilo, alquilarilo, alquilheteroarilo, arilalquilo y heteroarilalquilo, se refiere a una sustitucion por uno o mas grupos alquilo, arilo, heteroarilo, halo, -OR' y -NR'Rö, o sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85607906P | 2006-11-02 | 2006-11-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079840A2 true AR079840A2 (es) | 2012-02-22 |
Family
ID=39233054
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104876A AR063451A1 (es) | 2006-11-02 | 2007-11-01 | Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas. |
| ARP110100026A AR079840A2 (es) | 2006-11-02 | 2011-01-05 | Receptor nicotinico de acetilcolina, subtipo selectivo de amidas de diazabicicloalcanos |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104876A AR063451A1 (es) | 2006-11-02 | 2007-11-01 | Diazabiciclo alcanos como receptores nicotinicos de acetilcolina. composiciones farmaceuticas. |
Country Status (32)
| Country | Link |
|---|---|
| US (6) | US8114889B2 (es) |
| EP (2) | EP2284171B1 (es) |
| JP (2) | JP5539723B2 (es) |
| KR (2) | KR20100124356A (es) |
| CN (4) | CN101528745B (es) |
| AR (2) | AR063451A1 (es) |
| AT (2) | ATE545646T1 (es) |
| AU (2) | AU2007317433B2 (es) |
| BR (2) | BRPI0722387A2 (es) |
| CA (1) | CA2663925C (es) |
| CL (1) | CL2007003155A1 (es) |
| CO (1) | CO6180435A2 (es) |
| CY (1) | CY1112374T1 (es) |
| DK (1) | DK2094703T3 (es) |
| ES (2) | ES2395157T3 (es) |
| HR (1) | HRP20110570T1 (es) |
| IL (2) | IL197618A (es) |
| MX (1) | MX2009004801A (es) |
| MY (2) | MY145602A (es) |
| NO (1) | NO20091251L (es) |
| NZ (2) | NZ587847A (es) |
| PE (2) | PE20110671A1 (es) |
| PL (1) | PL2094703T3 (es) |
| PT (1) | PT2094703E (es) |
| RS (1) | RS51834B (es) |
| RU (2) | RU2448969C2 (es) |
| SA (1) | SA07280584B1 (es) |
| SI (1) | SI2094703T1 (es) |
| TW (3) | TWI404532B (es) |
| UA (2) | UA98944C2 (es) |
| UY (1) | UY30686A1 (es) |
| WO (1) | WO2008057938A1 (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI404532B (zh) * | 2006-11-02 | 2013-08-11 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
| AU2009221860A1 (en) * | 2008-03-05 | 2009-09-11 | Targacept, Inc. | Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloal kanes |
| WO2009113950A1 (en) * | 2008-03-10 | 2009-09-17 | Astrazeneca Ab | Therapeutic combinations of (a) an antipsychotic and (b) an alpha-4/beta-2 (a4b2)-neuronal nicotinic receptor agonist |
| WO2009147190A1 (en) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | Novel compounds |
| EP2280705B1 (en) | 2008-06-05 | 2014-10-08 | Glaxo Group Limited | Novel compounds |
| ES2445199T3 (es) | 2008-06-05 | 2014-02-28 | Glaxo Group Limited | Derivados de benzpirazol como inhibidores de PI3-quinasas |
| WO2010028011A1 (en) * | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclononanes and uses thereof |
| CN102143963A (zh) * | 2008-09-05 | 2011-08-03 | 塔加西普特公司 | 二氮杂双环辛烷的酰胺及其应用 |
| WO2010080757A2 (en) | 2009-01-07 | 2010-07-15 | Astrazeneca Ab | Combinations with an alpha-4beta-2 nicotinic agonist |
| US8524751B2 (en) | 2009-03-09 | 2013-09-03 | GlaxoSmithKline Intellecutual Property Development | 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases |
| ES2876933T3 (es) | 2009-04-30 | 2021-11-15 | Glaxo Group Ltd | Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas |
| RU2417082C2 (ru) * | 2009-07-14 | 2011-04-27 | Учреждение Российской Академии Наук Институт Физиологически Активных Веществ Ран (Ифав Ран) | Средство для восстановления утраченной памяти в норме и патологии у пациентов всех возрастных групп на основе n, n'-замещенных 3, 7-диазабицикло[3.3.1]нонанов, фармацевтическая композиция на его основе и способ ее применения |
| JP5536227B2 (ja) | 2009-11-18 | 2014-07-02 | スヴェン・ライフ・サイエンシズ・リミテッド | α４β２ニコチン性アセチルコリン受容体リガンドとしての二環式化合物 |
| DK2519514T3 (en) | 2009-12-29 | 2015-11-16 | Suven Life Sciences Ltd | Neuronal nicotinic alpha4beta2-acetylcholine receptor ligands |
| GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| PE20160845A1 (es) | 2013-11-26 | 2016-09-10 | Hoffmann La Roche | Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo |
| HUE046820T2 (hu) | 2014-03-26 | 2020-03-30 | Hoffmann La Roche | Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként |
| CN107106542B (zh) | 2014-10-20 | 2020-05-08 | 奥伊斯特普安生物制药公司 | 治疗眼部病状的方法 |
| MX377277B (es) | 2015-09-04 | 2025-03-07 | Hoffmann La Roche | Derivados de fenoximetilo. |
| RU2725138C2 (ru) | 2015-09-24 | 2020-06-30 | Ф. Хоффманн-Ля Рош Аг | Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca) |
| WO2017050732A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
| BR112018006034A2 (pt) | 2015-09-24 | 2018-10-09 | Hoffmann La Roche | compostos bicíclicos como inibidores de atx |
| MA42923A (fr) | 2015-09-24 | 2021-04-28 | Hoffmann La Roche | Composés bicycliques comme inhibiteurs mixtes de atx/ca |
| NZ746468A (en) | 2016-04-07 | 2023-06-30 | Oyster Point Pharma Inc | Methods of treating ocular conditions |
| KR20190129924A (ko) | 2017-03-16 | 2019-11-20 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물 |
| CN110382484B (zh) | 2017-03-16 | 2022-12-06 | 豪夫迈·罗氏有限公司 | 新的作为atx抑制剂的二环化合物 |
| ES2747768T3 (es) | 2017-03-20 | 2020-03-11 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR) |
| WO2020061378A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020061255A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| US20220378756A1 (en) | 2019-09-19 | 2022-12-01 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
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