AR072510A1 - Derivados de triazinas y de uracilos, su preparacion y su aplicacion en terapeutica humana - Google Patents
Derivados de triazinas y de uracilos, su preparacion y su aplicacion en terapeutica humanaInfo
- Publication number
- AR072510A1 AR072510A1 ARP090102680A ARP090102680A AR072510A1 AR 072510 A1 AR072510 A1 AR 072510A1 AR P090102680 A ARP090102680 A AR P090102680A AR P090102680 A ARP090102680 A AR P090102680A AR 072510 A1 AR072510 A1 AR 072510A1
- Authority
- AR
- Argentina
- Prior art keywords
- linear
- branched
- alkyl
- phenyl
- groups
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- 150000003918 triazines Chemical class 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 2
- 108090000790 Enzymes Proteins 0.000 abstract 2
- AEDMQUAPBVOJNN-UHFFFAOYSA-N [3-[2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl]-1,2,4-oxadiazol-5-yl]methanol Chemical compound O1C(CO)=NC(C=2SC(=NC=2)N2CCC(CC2)OC=2C(=CC=CC=2)C(F)(F)F)=N1 AEDMQUAPBVOJNN-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 150000002825 nitriles Chemical class 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- -1 vinyl methylsulfanyl Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- UUFQTNFCRMXOAE-UHFFFAOYSA-N 1-methylmethylene Chemical compound C[CH] UUFQTNFCRMXOAE-UHFFFAOYSA-N 0.000 abstract 1
- SSPYSWLZOPCOLO-UHFFFAOYSA-N 6-azauracil Chemical class O=C1C=NNC(=O)N1 SSPYSWLZOPCOLO-UHFFFAOYSA-N 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 101100167062 Caenorhabditis elegans chch-3 gene Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 abstract 1
- 125000005596 alkyl carboxamido group Chemical group 0.000 abstract 1
- 125000003435 aroyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 125000000490 cinnamyl group Chemical group C(C=CC1=CC=CC=C1)* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005117 dialkylcarbamoyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07D403/02—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
-
- 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
- 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
- A61P17/08—Antiseborrheics
-
- 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
- A61P17/10—Anti-acne 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Composiciones farmacéuticas y usos como inhibidores de la enzima SCD-1. Reivindicacion 1: Derivados de la 2H-[1,2,4]triazin-3,5-diona y de la H-pirimidin-2,4-diona para su uso como inhibidores de la actividad de la enzima SCD-1 y que corresponden a la formula general (1), en la que: W representa el nitrogeno o CH; R1 y R2 representan independientemente uno del otro: i) un hidrogeno o un radical alquilo o alquenilo lineal o ramificado en C1-7, o ii) un radical alquilo en C1-3 sustituido con unos grupos tales como: trifluorometilo, nitrilo, hidroxi, alcoxi en C1-3; alcoxialcoxi en C3-6, indolilo, tiofenilo, oxotiofenilo, N-alquilo o N-dialquilcarbamoilo en C1-3 o, fenilo o aroilo o benciloxi o N-arilcarbamoilo (para los cuales el nucleo fenilo está eventualmente sustituido con uno o varios grupos tales como alquilo lineal o ramificado en C1-4, nitro, halogeno), iii) un grupo fenilo o piridilo o naftilo o tiofenilo eventualmente sustituido con uno o varios grupos tales como halogeno, nitro, nitrilo, trifluorometilo, vinilo metilsulfanilo, alquilo lineal o ramificado en C1-4, alcoxi lineal o ramificado en C1-3, fenilo, N-mono o dialquilcarbamoilo en C1-3, alquilcarboxamido en C1-4, iv) un radical 2-oxocicloalquilo en C5-6 eventualmente condensado con un grupo fenilo; m es igual a 0 o 1; V representa CH2, CHCH3 o C=O; cuando n = 1, X-Y representa -N-(C=O)-, -N-CH2-, -CH-CH2-, -CH-O-, CH-(C=O)-, Z representa un grupo fenilo eventualmente sustituido con uno o varios grupos trifluorometilo, halogeno, alquilo lineal o ramificado en C1-4, alcoxi lineal o ramificado en C1-3; cuando n = 0, X representa N, Z representa un grupo fenilo o cinnamilo o ariloxicarbonilo o 2-fenilacetilo (cuya posicion 2 está eventualmente sustituida por un alcoilo lineal o ramificado en C1-4) para los cuales el aromático está eventualmente sustituido con uno o varios grupos trifluorometilo, halogeno, alquilo lineal o ramificado en C1-4, alcoxi lineal o ramificado en C1-3, nitro; así como las sales de adicion con las bases y los ácidos farmacéuticamente aceptables, y los diferentes enantiomeros de los compuestos que poseen unos carbonos asimétricos, así como sus mezclas en cualquier proporcion que comprenden en particular las mezclas racémicas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0854794A FR2933979B1 (fr) | 2008-07-15 | 2008-07-15 | Derives de triazines et uraciles, leur preparation et leur application en therapeutique humaine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072510A1 true AR072510A1 (es) | 2010-09-01 |
Family
ID=40394394
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102680A AR072510A1 (es) | 2008-07-15 | 2009-07-15 | Derivados de triazinas y de uracilos, su preparacion y su aplicacion en terapeutica humana |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8618287B2 (es) |
| EP (1) | EP2328886B1 (es) |
| JP (1) | JP5599788B2 (es) |
| AR (1) | AR072510A1 (es) |
| FR (1) | FR2933979B1 (es) |
| TW (1) | TW201006815A (es) |
| WO (1) | WO2010006962A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8648073B2 (en) | 2009-12-30 | 2014-02-11 | Fochon Pharma, Inc. | Certain dipeptidyl peptidase inhibitors |
| FR2958935B1 (fr) | 2010-04-19 | 2012-06-22 | Pf Medicament | Derives d'heterocycles azotes, leur preparation et leur application en therapeutique humaine |
| CN104803971B (zh) * | 2014-01-24 | 2021-11-30 | 深圳信立泰药业股份有限公司 | 化合物A单苯甲酸盐的晶型α及其制备方法和含有该晶型的药物组合物 |
| CN105017213B (zh) * | 2014-04-30 | 2017-11-14 | 成都苑东生物制药股份有限公司 | 尿嘧啶衍生物 |
| JP6814730B2 (ja) | 2014-09-05 | 2021-01-20 | ジェネンテック, インコーポレイテッド | 治療用化合物およびその使用 |
| CN117777121A (zh) | 2016-10-24 | 2024-03-29 | 詹森药业有限公司 | 化合物及其用途 |
| KR20190108118A (ko) | 2017-01-06 | 2019-09-23 | 유마니티 테라퓨틱스, 인크. | 신경계 장애의 치료를 위한 방법 |
| WO2019084157A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES THEREOF |
| JP7517992B2 (ja) | 2018-03-23 | 2024-07-17 | ヤンセン ファーマシューティカ エヌ.ベー. | 化合物及びその使用 |
| TWI884745B (zh) * | 2018-10-12 | 2025-05-21 | 美商拓臻股份有限公司 | 甲狀腺素受體β促效劑化合物 |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| BR112021014583A2 (pt) | 2019-01-24 | 2021-10-05 | Yumanity Therapeutics, Inc. | Compostos e utilizações dos mesmos |
| EP4017875A4 (en) | 2019-08-23 | 2023-05-03 | Terns Pharmaceuticals, Inc. | THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS |
| JP2022548250A (ja) | 2019-09-12 | 2022-11-17 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | 甲状腺ホルモン受容体ベータアゴニスト化合物 |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| WO2021104288A1 (zh) | 2019-11-26 | 2021-06-03 | 昆药集团股份有限公司 | 1,2,4-三嗪-3,5-二酮类化合物及其制备方法和应用 |
| WO2024102455A1 (en) * | 2022-11-09 | 2024-05-16 | Emory University | Non-covalent inhibitors of coronavirus main protease |
| US20240398794A1 (en) | 2023-04-07 | 2024-12-05 | Terns Pharmaceuticals, Inc. | COMBINATIONS OF GLP-1R AND THRß AGONISTS AND METHODS OF USE THEREOF |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5973573A (ja) * | 1982-09-09 | 1984-04-25 | ワ−ナ−−ランバ−ト・コンパニ− | ジアミノピリミジン化合物 |
| JP2006506451A (ja) * | 2002-10-11 | 2006-02-23 | アストラゼネカ アクチボラグ | 1,4−ジ置換ピペリジン誘導体および11−βHSD1阻害薬としてのそれらの使用 |
| FR2866339B1 (fr) * | 2004-02-18 | 2006-05-05 | Pf Medicament | Derives de 1,2,4-triazines, leur preparation et leur application en therapeutique humaine |
| TW200609219A (en) * | 2004-06-17 | 2006-03-16 | Neurogen Corp | Aryl-substituted piperazine derivatives |
| CA2632936A1 (en) * | 2005-12-20 | 2007-06-28 | Merck Frosst Canada Ltd. | Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
-
2008
- 2008-07-15 FR FR0854794A patent/FR2933979B1/fr not_active Expired - Fee Related
-
2009
- 2009-07-07 EP EP09797466.1A patent/EP2328886B1/en not_active Not-in-force
- 2009-07-07 WO PCT/EP2009/058609 patent/WO2010006962A1/en not_active Ceased
- 2009-07-07 US US13/054,293 patent/US8618287B2/en not_active Expired - Fee Related
- 2009-07-07 JP JP2011517863A patent/JP5599788B2/ja not_active Expired - Fee Related
- 2009-07-10 TW TW098123438A patent/TW201006815A/zh unknown
- 2009-07-15 AR ARP090102680A patent/AR072510A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP5599788B2 (ja) | 2014-10-01 |
| FR2933979B1 (fr) | 2012-08-24 |
| US20110118266A1 (en) | 2011-05-19 |
| FR2933979A1 (fr) | 2010-01-22 |
| WO2010006962A1 (en) | 2010-01-21 |
| TW201006815A (en) | 2010-02-16 |
| US8618287B2 (en) | 2013-12-31 |
| EP2328886B1 (en) | 2016-12-28 |
| EP2328886A1 (en) | 2011-06-08 |
| JP2011528007A (ja) | 2011-11-10 |
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