RU2010150615A - Пролекарства антагонистов а2в рецептора аденозина - Google Patents
Пролекарства антагонистов а2в рецептора аденозина Download PDFInfo
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- RU2010150615A RU2010150615A RU2010150615/04A RU2010150615A RU2010150615A RU 2010150615 A RU2010150615 A RU 2010150615A RU 2010150615/04 A RU2010150615/04 A RU 2010150615/04A RU 2010150615 A RU2010150615 A RU 2010150615A RU 2010150615 A RU2010150615 A RU 2010150615A
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- methyl
- phenyl
- disease state
- pyrazol
- dioxo
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- 102000009346 Adenosine receptors Human genes 0.000 title 1
- 108050000203 Adenosine receptors Proteins 0.000 title 1
- 201000010099 disease Diseases 0.000 claims abstract 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 10
- -1 1 - {[3- (trifluoromethyl) phenyl] methyl} pyrazol-4-yl Chemical group 0.000 claims abstract 6
- 125000000217 alkyl group Chemical group 0.000 claims abstract 6
- 241000124008 Mammalia Species 0.000 claims abstract 4
- 208000006673 asthma Diseases 0.000 claims abstract 4
- 150000001875 compounds Chemical class 0.000 claims abstract 4
- 210000001035 gastrointestinal tract Anatomy 0.000 claims abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 4
- 239000001257 hydrogen Substances 0.000 claims abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 3
- 201000001320 Atherosclerosis Diseases 0.000 claims abstract 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims abstract 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims abstract 2
- 206010012735 Diarrhoea Diseases 0.000 claims abstract 2
- 206010028980 Neoplasm Diseases 0.000 claims abstract 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims abstract 2
- CHXVYXIMUQHSRC-UHFFFAOYSA-N [3-ethyl-2,6-dioxo-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]purin-7-yl] 2,2-dimethylbutanoate Chemical compound CCC(C(=O)ON1C(=NC=2N(C(N(C(C1=2)=O)CCC)=O)CC)C=1C=NN(C=1)CC1=CC(=CC=C1)C(F)(F)F)(C)C CHXVYXIMUQHSRC-UHFFFAOYSA-N 0.000 claims abstract 2
- HOLLSHYBSWZLEY-UHFFFAOYSA-N [3-ethyl-2,6-dioxo-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]purin-7-yl] 2-methylbutanoate Chemical compound CCC(C)C(=O)ON1C=2C(=O)N(CCC)C(=O)N(CC)C=2N=C1C(=C1)C=NN1CC1=CC=CC(C(F)(F)F)=C1 HOLLSHYBSWZLEY-UHFFFAOYSA-N 0.000 claims abstract 2
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims abstract 2
- 230000033115 angiogenesis Effects 0.000 claims abstract 2
- 201000011510 cancer Diseases 0.000 claims abstract 2
- 208000027866 inflammatory disease Diseases 0.000 claims abstract 2
- 230000002757 inflammatory effect Effects 0.000 claims abstract 2
- CAAULPUQFIIOTL-UHFFFAOYSA-N methyl dihydrogen phosphate Chemical compound COP(O)(O)=O CAAULPUQFIIOTL-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 229940121359 adenosine receptor antagonist Drugs 0.000 claims 1
- 239000000296 purinergic P1 receptor antagonist Substances 0.000 claims 1
- 229940123053 Adenosine A2b receptor antagonist Drugs 0.000 abstract 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
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- Urology & Nephrology (AREA)
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- Rheumatology (AREA)
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Abstract
1. Способ лечения болезненного состояния у млекопитающего, которое поддается лечению антагонистом А2В рецептора аденозина, включающий введение млекопитающему терапевтически эффективной дозы соединения формулы I: ! ! в которой R1 и R2 независимо обозначают низший алкил; ! R4 обозначает в случае необходимости замещенный фенил; ! X обозначает водород или метил; и ! Y обозначает -С(О)R, где R обозначает в случае необходимости замещенный низший алкил; или ! Y обозначает -P(О)(OR5)2, где R5 обозначает водород или низший алкил; ! или его фармацевтически приемлемая соль. ! 2. Способ по п.1, в котором соединение по п.1 выбрано из группы, состоящей из [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-троигидропурин-7-ил]метилацетата, [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-тригидропурин-7-ил]метилбутаноата, [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-тригидропурин-7-ил]метил-2,2-диметилпропаноата и [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)(1,3,7-тригидропурин-7-ил)]метилдигидрофосфата. ! 3. Способ по п.1, в котором болезненное состояние выбирают из атеросклероза, ангиогенеза, диабетической ретинопатии, рака, хронического обструктивного заболевания легких и астмы. ! 4. Способ по п.3, в котором болезненное состояние представляет собой астму. ! 5. Способ по п.1, в котором болезненное состояние представляет собой воспалительное нарушение желудочно-кишечного тракта. ! 6. Способ по п.5, в котором воспалительное нарушение желудочно-кишечного тракта представляет собой диарею. ! 7. Способ по п.1, в котором болезненное состояние представляет собой неврологи�
Claims (8)
1. Способ лечения болезненного состояния у млекопитающего, которое поддается лечению антагонистом А2В рецептора аденозина, включающий введение млекопитающему терапевтически эффективной дозы соединения формулы I:
в которой R1 и R2 независимо обозначают низший алкил;
R4 обозначает в случае необходимости замещенный фенил;
X обозначает водород или метил; и
Y обозначает -С(О)R, где R обозначает в случае необходимости замещенный низший алкил; или
Y обозначает -P(О)(OR5)2, где R5 обозначает водород или низший алкил;
или его фармацевтически приемлемая соль.
2. Способ по п.1, в котором соединение по п.1 выбрано из группы, состоящей из [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-троигидропурин-7-ил]метилацетата, [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-тригидропурин-7-ил]метилбутаноата, [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)-1,3,7-тригидропурин-7-ил]метил-2,2-диметилпропаноата и [3-этил-2,6-диоксо-1-пропил-8-(1-{[3-(трифторметил)фенил]метил}пиразол-4-ил)(1,3,7-тригидропурин-7-ил)]метилдигидрофосфата.
3. Способ по п.1, в котором болезненное состояние выбирают из атеросклероза, ангиогенеза, диабетической ретинопатии, рака, хронического обструктивного заболевания легких и астмы.
4. Способ по п.3, в котором болезненное состояние представляет собой астму.
5. Способ по п.1, в котором болезненное состояние представляет собой воспалительное нарушение желудочно-кишечного тракта.
6. Способ по п.5, в котором воспалительное нарушение желудочно-кишечного тракта представляет собой диарею.
7. Способ по п.1, в котором болезненное состояние представляет собой неврологическое нарушение.
8. Способ по п.7, в котором неврологическое нарушение представляет собой сенильную деменцию, болезнь Альцгеймера или болезнь Паркинсона.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69140805P | 2005-06-16 | 2005-06-16 | |
| US60/691,408 | 2005-06-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007146669/04A Division RU2415858C2 (ru) | 2005-06-16 | 2006-06-14 | Пролекарства антагонистов a2b рецептора аденозина |
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| RU2010150615A true RU2010150615A (ru) | 2012-06-20 |
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| RU2007146669/04A RU2415858C2 (ru) | 2005-06-16 | 2006-06-14 | Пролекарства антагонистов a2b рецептора аденозина |
| RU2010150615/04A RU2010150615A (ru) | 2005-06-16 | 2010-12-09 | Пролекарства антагонистов а2в рецептора аденозина |
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| RU2007146669/04A RU2415858C2 (ru) | 2005-06-16 | 2006-06-14 | Пролекарства антагонистов a2b рецептора аденозина |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US7625881B2 (ru) |
| EP (2) | EP2301937A1 (ru) |
| JP (1) | JP5044823B2 (ru) |
| KR (1) | KR20080016645A (ru) |
| CN (1) | CN101198608B (ru) |
| AU (1) | AU2006259411B2 (ru) |
| CA (1) | CA2612344A1 (ru) |
| IL (1) | IL188103A0 (ru) |
| MX (1) | MX2007015909A (ru) |
| NO (1) | NO20080278L (ru) |
| NZ (1) | NZ564326A (ru) |
| RU (2) | RU2415858C2 (ru) |
| WO (1) | WO2006138376A1 (ru) |
| ZA (1) | ZA200710878B (ru) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080194593A1 (en) * | 2001-11-09 | 2008-08-14 | Rao Kalla | A2b adenosine receptor antagonists |
| US7317017B2 (en) | 2002-11-08 | 2008-01-08 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US20080318983A1 (en) * | 2001-11-09 | 2008-12-25 | Rao Kalla | A2b adenosine receptor antagonists |
| AU2004268964B2 (en) * | 2003-08-25 | 2010-03-11 | Allergan Sales, Llc | Substituted 8-heteroaryl xanthines |
| NZ589657A (en) | 2004-10-15 | 2012-06-29 | Gilead Palo Alto Inc | Method of preventing and treating airway remodeling and pulmonary inflammation using A2B adenosine receptor antagonists |
| US7579348B2 (en) * | 2005-02-25 | 2009-08-25 | Pgxhealth, Llc | Derivatives of 8-substituted xanthines |
| US7618962B2 (en) * | 2005-02-25 | 2009-11-17 | Pgx Health, Llc | Pyrazolyl substituted xanthines |
| WO2006091936A2 (en) | 2005-02-25 | 2006-08-31 | Adenosine Therapeutics, Llc | Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines |
| EP2301937A1 (en) | 2005-06-16 | 2011-03-30 | Cv Therapeutics, Inc. | Prodrugs of A2b adenosine receptor antagonists |
| US7795268B2 (en) * | 2006-03-17 | 2010-09-14 | Gilead Palo Alto, Inc. | Method of treating hepatic disease using A2B adenosine receptor antagonists |
| US7884100B2 (en) * | 2006-06-16 | 2011-02-08 | Pgxhealth, Llc | Substituted 8-[6-amino-3-pyridyl]xanthines |
| US7767685B2 (en) * | 2006-06-29 | 2010-08-03 | King Pharmaceuticals Research And Development, Inc. | Adenosine A2B receptor antagonists |
| WO2009088518A1 (en) * | 2008-01-11 | 2009-07-16 | Cv Therapeutics, Inc. | A2b adenosine receptor antagonists for the treatment of cancer |
| WO2009157938A1 (en) * | 2008-06-26 | 2009-12-30 | Cv Therapeutics, Inc. | A2b adenosine receptor antagonists for treating cancer |
| AU2010339691B2 (en) | 2010-01-07 | 2015-04-02 | Alkermes Pharma Ireland Limited | Prodrugs of heteraromatic compounds |
| CN103237548A (zh) * | 2010-06-30 | 2013-08-07 | 吉利德科学股份有限公司 | A2b腺苷受体拮抗剂用于治疗肺高血压的应用 |
| EP2616470B1 (en) | 2010-09-13 | 2016-10-12 | Advinus Therapeutics Limited | Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications |
| AR085942A1 (es) | 2011-04-07 | 2013-11-06 | Gilead Sciences Inc | Uso de receptor de aadenosina para tratar la insuficiencia cardiaca y la arritmia en pacientes posinfarto de miocardio |
| JP2014514300A (ja) * | 2011-04-08 | 2014-06-19 | スファエラ ファーマ ピーティーイー リミテッド | 置換メチルホルミル試薬並びに化合物の物理化学的性質及び／又は薬物動態学的性質を改質するためのそれらの使用方法 |
| ES2656087T3 (es) | 2012-06-08 | 2018-02-23 | Gilead Sciences, Inc. | Inhibidores macrocíclicos de virus Flaviviridae |
| AR091279A1 (es) | 2012-06-08 | 2015-01-21 | Gilead Sciences Inc | Inhibidores macrociclicos de virus flaviviridae |
| JP6209601B2 (ja) | 2012-06-08 | 2017-10-04 | ギリアード サイエンシーズ， インコーポレイテッド | フラビウイルス科ウイルスの大環状阻害剤 |
| ES2580702B1 (es) | 2015-02-25 | 2017-06-08 | Palobiofarma, S.L. | Derivados de 2-aminopiridina como antagonistas del receptor A2b de adenosina y ligandos del receptor MT3 de melatonina |
| US10308671B2 (en) * | 2015-12-14 | 2019-06-04 | Max-Planck-Gesellschaft Zur Forderung | Water-soluble derivatives of 3,5-diphenyl-diazole compounds |
| CA3093234A1 (en) | 2018-03-05 | 2019-09-12 | Teon Therapeutics, Inc. | Adenosine receptor antagonists and uses thereof |
| JP7156154B2 (ja) * | 2019-04-18 | 2022-10-19 | 株式会社島津製作所 | 培地処理システム及び培地処理方法 |
| TW202327612A (zh) * | 2021-09-10 | 2023-07-16 | 美商天恩治療有限公司 | 使用腺苷受體拮抗劑之改良療法 |
Family Cites Families (29)
| 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 |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| US6117878A (en) * | 1998-02-24 | 2000-09-12 | University Of Virginia | 8-phenyl- or 8-cycloalkyl xanthine antagonists of A2B human adenosine receptors |
| US6815446B1 (en) * | 1999-08-31 | 2004-11-09 | Vanderbilt University | Selective antagonists of A2B adenosine receptors |
| EP1255550A2 (en) * | 2000-02-17 | 2002-11-13 | Cv Therapeutics, Inc. | Method for identifying and using a 2b adenosine receptor antagonists to mediate mammalian cell proliferation |
| US6387913B1 (en) * | 2000-12-07 | 2002-05-14 | S. Jamal Mustafa | Method of treating airway diseases with combined administration of A2B and A3 adenosine receptor antagonists |
| US20030235555A1 (en) * | 2002-04-05 | 2003-12-25 | David Shealey | Asthma-related anti-IL-13 immunoglobulin derived proteins, compositions, methods and uses |
| CN100467469C (zh) * | 2001-11-09 | 2009-03-11 | Cv医药有限公司 | A2b腺苷受体拮抗剂 |
| US7125993B2 (en) * | 2001-11-09 | 2006-10-24 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US7317017B2 (en) * | 2002-11-08 | 2008-01-08 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US7304070B2 (en) * | 2001-11-09 | 2007-12-04 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US20080318983A1 (en) * | 2001-11-09 | 2008-12-25 | Rao Kalla | A2b adenosine receptor antagonists |
| US6977300B2 (en) | 2001-11-09 | 2005-12-20 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| WO2003053366A2 (en) * | 2001-12-20 | 2003-07-03 | Osi Pharmaceuticals, Inc. | Pyrimidine a2b selective antagonist compounds, their synthesis and use |
| EP1601649A4 (en) * | 2003-02-19 | 2009-03-04 | Endacea Inc | A1-adenosine receptor antagonistic |
| DK1622908T3 (da) * | 2003-05-06 | 2008-11-17 | Cv Therapeutics Inc | Xanthin-derivater som A2B adenosin-receptor-antagonister |
| AU2004268964B2 (en) * | 2003-08-25 | 2010-03-11 | Allergan Sales, Llc | Substituted 8-heteroaryl xanthines |
| MXPA06004789A (es) * | 2003-10-31 | 2006-07-03 | Cv Therapeutics Inc | Antagonistas del receptor de adenosina a2b. |
| SI1789053T1 (sl) * | 2004-09-01 | 2012-09-28 | Gilead Sciences Inc | Postopek celjenja rane z uporabo antagonistov A2B adenozinskih receptorjev |
| NZ589657A (en) * | 2004-10-15 | 2012-06-29 | Gilead Palo Alto Inc | Method of preventing and treating airway remodeling and pulmonary inflammation using A2B adenosine receptor antagonists |
| EP2301937A1 (en) * | 2005-06-16 | 2011-03-30 | Cv Therapeutics, Inc. | Prodrugs of A2b adenosine receptor antagonists |
| US7795268B2 (en) * | 2006-03-17 | 2010-09-14 | Gilead Palo Alto, Inc. | Method of treating hepatic disease using A2B adenosine receptor antagonists |
| ES2437871T3 (es) * | 2006-07-07 | 2014-01-14 | Gilead Sciences, Inc. | Moduladores del receptor tipo toll 7 |
| CN102015712A (zh) * | 2008-03-26 | 2011-04-13 | 阿德维纳斯治疗私人有限公司 | 作为腺苷受体拮抗剂的杂环化合物 |
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- 2006-06-14 CA CA002612344A patent/CA2612344A1/en not_active Abandoned
- 2006-06-14 CN CN2006800213389A patent/CN101198608B/zh not_active Expired - Fee Related
- 2006-06-14 MX MX2007015909A patent/MX2007015909A/es active IP Right Grant
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- 2006-06-14 KR KR1020077029351A patent/KR20080016645A/ko not_active Application Discontinuation
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| US20100056538A1 (en) | 2010-03-04 |
| CA2612344A1 (en) | 2006-12-28 |
| JP5044823B2 (ja) | 2012-10-10 |
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| ZA200710878B (en) | 2009-05-27 |
| AU2006259411A1 (en) | 2006-12-28 |
| US20110160162A1 (en) | 2011-06-30 |
| US7625881B2 (en) | 2009-12-01 |
| EP1891070A1 (en) | 2008-02-27 |
| MX2007015909A (es) | 2008-03-06 |
| US8143249B2 (en) | 2012-03-27 |
| CN101198608A (zh) | 2008-06-11 |
| NZ564326A (en) | 2010-01-29 |
| IL188103A0 (en) | 2008-03-20 |
| RU2415858C2 (ru) | 2011-04-10 |
| JP2008543860A (ja) | 2008-12-04 |
| NO20080278L (no) | 2008-02-28 |
| CN101198608B (zh) | 2011-04-27 |
| RU2007146669A (ru) | 2009-06-20 |
| US20060293283A1 (en) | 2006-12-28 |
| AU2006259411B2 (en) | 2012-03-22 |
| KR20080016645A (ko) | 2008-02-21 |
| EP2301937A1 (en) | 2011-03-30 |
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