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环戊丙酸睾酮 | 58-20-8

中文名称
环戊丙酸睾酮
中文别名
环戊丙酸睾丸素;1-睾酮环戊丙酸酯;USP限制环戊丙酸睾酮
英文名称
testosterone cypionate
英文别名
Testosterone cyclopentylpropionate;testosterone 17β-cypionate;depo-testosterone;Deposteron;17β-(3-cyclopentyl-propionyloxy)-androst-4-en-3-one;17β-(3-Cyclopentyl-propionyloxy)-androst-4-en-3-on;[(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 3-cyclopentylpropanoate
环戊丙酸睾酮化学式
CAS
58-20-8
化学式
C27H40O3
mdl
MFCD00053944
分子量
412.613
InChiKey
HPFVBGJFAYZEBE-ZLQWOROUSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

物化性质

  • 熔点:
    101-102°
  • 比旋光度:
    D25 +87° (CHCl3)
  • 沸点:
    492.01°C (rough estimate)
  • 密度:
    0.9795 (rough estimate)
  • 溶解度:
    DMF:25mg/mL; DMSO:5mg/mL;乙醇:15mg/mL;乙醇:PBS (pH 7.2)(1:2): 0.3 mg/mL

计算性质

  • 辛醇/水分配系数(LogP):
    6.4
  • 重原子数:
    30
  • 可旋转键数:
    5
  • 环数:
    5.0
  • sp3杂化的碳原子比例:
    0.851
  • 拓扑面积:
    43.4
  • 氢给体数:
    0
  • 氢受体数:
    3

ADMET

代谢
为了开始其活动,睾酮环戊丙酸酯需要通过血液中的酶进行处理。这些酶将环戊丙酸酯基团与睾酮之间的键断开。一旦分离,睾酮就通过两条不同的途径被代谢成17-酮类固醇。主要活性代谢物是雌二醇和二氢睾酮(DHT)。睾酮在皮肤、肝脏和泌尿生殖道中通过类固醇5α-还原酶被代谢成DHT。在生殖组织中,DHT进一步被代谢成雄烷二醇。
To start its activity, testosterone cypionate has to be processed by enzymes in the bloodstream. These enzymes will break the bond between the cypionate ester moiety and the testosterone. Once separated, testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT). Testosterone is metabolized to DHT by steroid 5α-reductase in skin, liver and urogenital tract. In reproductive tissues DHT is further metabolized to androstanediol.
来源:DrugBank
毒理性
  • 蛋白质结合
睾酮环己酸酯,在转化为睾酮后,大约有98%与血浆中的性激素结合球蛋白结合。
Testosterone cypionate, following conversion into testosterone, is approximately 98% protein-bound to sex hormone-binding globulin in plasma.
来源:DrugBank
吸收、分配和排泄
  • 吸收
Testosterone cypionate 是一种酯化的合成代谢类固醇,这使其在脂肪中具有更高的溶解度,因此,与同类分子相比,其释放和吸收速度较慢。200 毫克睾酮环戊丙酸酯的肌内注射产生的平均血药浓度峰值(Cmax)为1122 ng/dl,发生在注射后第4至5天。第五天后,血浆中的睾酮环戊丙酸酯水平下降,平均达到400 ng/dl。
Testosterone cypionate is an esterified anabolic which allows it to present a greater degree of solubility in fats and thus, the release and absorption occur in a slow rate compare to homologous molecules. Intramuscular administration of 200 mg of testosterone cypionate produced a mean supratherapeutic Cmax of 1122 ng/dl which occurred 4-5 days post-injection. After the fifth day, the levels of testosterone cypionate in plasma went down reaching an average of 400 ng/dl.
来源:DrugBank
吸收、分配和排泄
  • 消除途径
大约90%的肌肉内注射的睾酮剂量以睾酮及其代谢物的葡萄糖醛酸和硫酸结合物形式通过尿液排出;大约6%的剂量以未结合形式主要通过粪便排出。
About 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form.
来源:DrugBank
吸收、分配和排泄
  • 分布容积
静脉注射睾酮后的分布体积大约为每千克1升。
The volume of distribution following intravenous administration of testosterone is of approximately 1 L/kg.
来源:DrugBank
吸收、分配和排泄
  • 清除
睾酮环己丙酸酯与睾酮的其他类似物相比,在肌肉注射后的清除率较低。
Testosterone cypionate presents a lower clearance rate after intramuscular administration compared to other analogs of testosterone.
来源:DrugBank

安全信息

  • 危险品标志:
    T
  • 安全说明:
    S22,S26,S36,S53
  • 危险类别码:
    R45
  • WGK Germany:
    3
  • 海关编码:
    2937290018
  • 危险品运输编号:
    HAZARD
  • RTECS号:
    XA3066000
  • 储存条件:
    2-8°C

SDS

SDS:b3bc1744a30f0e142e56170cd1747a66
查看

Section 1. Chemical Product and Company Identification
Testosterone cypionate
Common Name/
Trade Name
Testosterone cypionate

Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at
least 15 minutes. Get medical attention if irritation occurs.
Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops.
Serious Skin Contact Not available.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get
medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an
unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen tight
clothing such as a collar, tie, belt or waistband.
Serious Ingestion Not available.

Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points CLOSED CUP: Higher than 93.3°C (200°F).
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2).
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances Non-flammable in presence of shocks.
Explosion Hazards in Presence Slightly explosive in presence of open flames and sparks.
Non-explosive in presence of shocks.
of Various Substances
SMALL FIRE: Use DRY chemical powder.
Fire Fighting Media
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
As with most organic solids, fire is possible at elevated temperatures. When heated to decomposition it emits
Special Remarks on
acrid smoke and irritating fumes.
Fire Hazards
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presences of an ignition source is a potential dust
Hazards explosion hazard.

Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water
on the contaminated surface and allow to evacuate through the sanitary system.
Testosterone cypionate

Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not
breathe dust. Wear suitable protective clothing. If you feel unwell, seek medical attention and show the label
when possible. Keep away from incompatibles such as oxidizing agents.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area. Sensitive to light. Store in
light-resistant containers.

Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (Crystalline powder) Odor Slight.
Taste Not available.
Molecular Weight 412.61 g/mole
Color White. Off-white.
pH (1% soln/water) Not applicable.
Not available.
Boiling Point
Melting Point 98°C (208.4°F) - 104 C.
Not available.
Critical Temperature
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties Not available.
Solubility Easily soluble in diethyl ether.
Insoluble in cold water, hot water.
Freely soluble in chloroform, dioxane, alcohol.

Section 10. Stability and Reactivity Data
Stability The product is stable.
Instability Temperature Not available.
Conditions of Instability Excess heat and incompatible materials
Incompatibility with various Reactive with oxidizing agents.
substances
Testosterone cypionate
Non-corrosive in presence of glass.
Corrosivity
Special Remarks on Sensitive to light.
Reactivity
Special Remarks on Not available.
Corrosivity
Will not occur.
Polymerization

Section 11. Toxicological Information
Routes of Entry Absorbed through skin. Inhalation. Ingestion.
Toxicity to Animals LD50: Not available.
LC50: Not available.
Chronic Effects on Humans TERATOGENIC EFFECTS: Classified POSSIBLE for human.
DEVELOPMENTAL TOXICITY: Classified Reproductive system/toxin/female, Reproductive system/toxin/male
[POSSIBLE].
May cause damage to the following organs: blood, the reproductive system, liver.
Other Toxic Effects on Slightly hazardous in case of skin contact (irritant, permeator), of ingestion, of inhalation.
Humans
Special Remarks on LD50 [Mouse] - Route: Intraperitoneal; Dose: >1000 mg/ kg
Toxicity to Animals
Special Remarks on May cause adverse reproductive effects and birth defects.
Chronic Effects on Humans May affect genetic material.
May cause cancer
Special Remarks on other Potential Effects of Overexposure:
Toxic Effects on Humans Anabolic steroid
Skin: May cause skin irritation. May be absorbed through skin
Eyes: Dust may cause eye irritation.
Inhalation: Dust may cause respiratory tract irritaiton.
Ingestion: May cause gastrointestinal tract irritation with upset stomach or stomach pain, nausea, vomiting,
diarrhea. May cause water and salt retention (edema), weight gain, acne and muscular development. Other
symptoms may include headache, unusual tiredness, dizziness, trouble sleeping, increased pubic hair growth,
change in sex drive. Females may also experience virilizing side effects such as facial hair, deepening of the
voice, and menstrual irregularities. Effects of chronic overexposure in women include male-pattern baldness,
excessive body hair, prominant musculature, and hypertrophy of the clitoris, decreased breast size, oily skin,
impaired fertility. Effects generally slowly subside on discontinuation of exposure, but with prolonged
overexposure in women some effects may become irreversible. Overexposure in males may lead to feminizing
side effects (breast enlargement and or soreness), and decreased spermatogenesis or impaired fertility due to
inhibition of gonadotropin secretion and metabolic conversion of androgens to estrogens. Other symptoms of
overexposure in males may include frequent or continuing erections, chills, pain in the scrotum or groin, difficulty
urinating, decreased testicle size, and aggressive behavior.
May also affect blood(clotting disorders, elevated cholesterol levels, change in red blood cell count), and liver.
Effects on the liver may cause yellowing of the skin or eyes (jaundice).
Chronic exposure may cause hypersensitization, masculinization in females, heart problems in males, impaired
fertility in males and females and cancer.
Medical Conditions Aggravated by Exposure: Hypersensitivity to material, males with breast or prostate cancer,
hypercalcemia resulting from osteolysis, pre-exisiting liver, kidney, or heart problems, and enlarged prostate gland.

Section 12. Ecological Information
Not available.
Ecotoxicity
Not available.
BOD5 and COD
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may
arise.
Toxicity of the Products The product itself and its products of degradation are not toxic.
of Biodegradation
Testosterone cypionate
Not available.
Special Remarks on the
Products of Biodegradation

Section 13. Disposal Considerations
Waste must be disposed of in accordance with federal, state and local environmental
Waste Disposal
control regulations.

Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
Identification
Special Provisions for Not applicable.
Transport
DOT (Pictograms)

Section 15. Other Regulatory Information and Pictograms
Federal and State California prop. 65: This product contains the following ingredients for which the State of California has found to
cause cancer, birth defects or other reproductive harm, which would require a warning under the statute:
Regulations
Testosterone cypionate
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause reproductive harm (female) which would require a warning under the statute: Testosterone cypionate
(Listed as Anabolic Steroid)
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause reproductive harm (male) which would require a warning under the statute: Testosterone cypionate (Listed
as Anabolic Steroid)
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause birth defects which would require a warning under the statute: Testosterone cypionate
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause cancer which would require a warning under the statute: Testosterone cypionate (List3ed as Testosterone
and its Esters)
California California prop. 65: This product contains the following ingredients for which the State of California has found
Proposition 65 to cause cancer which would require a warning under the statute: Testosterone cypionate
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has found
to cause birth defects which would require a warning under the statute: Testosterone cypionate
Other Regulations EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R45- May cause cancer. S36/37- Wear suitable protective clothing and
R63- Possible risk of harm to the gloves.
unborn child. S46- If swallowed, seek medical advice
immediately and show this container or label.
S53- Avoid exposure - obtain special
instructions before use.
Health Hazard
HMIS (U.S.A.) 1 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
1 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
Testosterone cypionate
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.
Testosterone cypionate
All chemicals may pose unknown hazards and should be used with caution. This Material Safety Data Sheet (MSDS) applies only to the material as packaged. If this product is
combined with other materials, deteriorates, or becomes contaminated, it may pose hazards not mentioned in this MSDS. It shall be the user's responsibility to develop proper
methods of handling and personal protection based on the actual conditions of use. While this MSDS is based on technical data judged to be reliable, Spectrum Quality Products,


SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

药理作用

内源性雄激素负责男性性器官的正常生长和发育,维持第二性征,包括前列腺、精囊、阴茎和阴囊的生长与成熟;促进男性特有的毛发分布,如胡须、耻骨、胸部及腋下毛发的发育;使喉头增大、声带增厚,并导致身体肌肉和脂肪分布的变化。这类药物还会引起氮、钠、钾和磷的滞留以及尿钙排泄减少。研究显示雄激素可促进蛋白质合成代谢,抑制蛋白质分解代谢。

内源性雄激素还负责青春期及最终生长突增的终止,这一过程由骨骺生长中心的融合所引发;在儿童中,外源性雄激素可以加速线性生长速率,但可能造成骨成熟不均匀。长期使用可能导致骨骺过早闭合和生长停止。

此外,雄激素还能刺激红细胞生成因子产生红细胞,并抑制垂体促黄体激素(LH)的释放以减少内源性睾酮分泌。

人工合成雄激素

环戊丙酸睾酮是一种人工合成的雄激素,在临床上主要用于治疗无睾症或类无睾症、功能性子宫出血、月经过多、子宫内膜异位症、子宫肌瘤、更年期综合征、转移性乳腺癌和卵巢癌、老年性骨质疏松以及再生障碍性贫血等。

药代动力学

环戊丙酸睾酮的极性小于游离睾酮。注射油中的睾酮酯通过肌肉内缓慢吸收,可在两到四周内给予一次。血浆中约98%的睾酮与特定的睾酮-雌二醇结合球蛋白结合,仅有2%为游离形式。

大约90%的剂量以葡萄糖醛酸和葡萄糖的结合物的形式经尿液排出体外;约6%的剂量通过未结合形式从粪便中排出。睾酮主要在肝脏失活,并通过两种途径代谢成各种17-酮类固醇。肌肉注射时,环戊丙酸睾酮的半衰期约为八天。

适应症
  1. 原发性性腺功能减退症(先天或后天):由于睾丸衰竭引起的隐睾症、双侧扭转、睾丸炎、睾丸消失综合征;或者因手术导致的睾丸切除术。
  2. 低促性腺功能减退症(先天或后天):由促性腺激素或LHRH缺陷,以及由肿瘤、创伤或放射造成的垂体-下丘脑损伤所引起的。

上下游信息

  • 上游原料
    中文名称 英文名称 CAS号 化学式 分子量
    睾酮 testosterone 58-22-0 C19H28O2 288.43
    —— 17-hydroxy-3-oxo-androst-4-ene-17-carbonitrile 17006-07-4 C20H27NO2 313.44
  • 下游产品
    中文名称 英文名称 CAS号 化学式 分子量
    睾酮 testosterone 58-22-0 C19H28O2 288.43

反应信息

  • 作为反应物:
    描述:
    环戊丙酸睾酮乙醇 为溶剂, 生成 睾酮
    参考文献:
    名称:
    大鼠睾丸激素及其酯衍生物的皮肤渗透。
    摘要:
    为了建立改善睾丸激素透皮递送的最佳条件,我们研究了睾丸激素酯衍生物的亲脂性与大鼠皮肤睾丸激素渗透率之间的关系。我们使用乙醇/水共溶剂系统进行了睾丸激素及其市售酯衍生物,半胱氨酸睾丸酮,丙酸睾丸酮和17β-环丙酸睾丸酮的大鼠皮肤渗透研究。在37摄氏度下确定每种药物在乙醇/水系统的各种成分中饱和的水溶性和大鼠皮肤渗透率。随着乙醇体积分数的增加,睾丸酮及其酯衍生物的水溶性呈指数增加。 100%(v / v)。研究了丙酸睾丸酮在皮肤匀浆和提取物中的稳定性,以观察在皮肤渗透过程中酶的降解。发现丙酸睾丸酮在等渗缓冲液和表皮侧提取物中在37摄氏度下稳定10h。但是,在皮肤匀浆和真皮侧提取物中,丙酸睾丸酮会迅速降解产生睾丸激素,这意味着丙酸睾丸酮会迅速降解。在皮肤渗透过程中降解为睾丸激素。乙醇/水系统中睾丸激素的稳态渗透率随乙醇体积分数的增加呈指数增加,在70%时达到最大值(2.69 +/- 0.69 microg
    DOI:
    10.1211/0022357001774101
  • 作为产物:
    描述:
    3-ethoxy-17β-(3-cyclopentyl-propionyloxy)-androsta-3,5-diene 在 盐酸丙酮 作用下, 生成 环戊丙酸睾酮
    参考文献:
    名称:
    An Improved Method of Preparing Testosterone, Dihydrotestosterone and Some of their Esters
    摘要:
    DOI:
    10.1021/ja01099a040
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文献信息

  • [EN] NOVEL N-SUBSTITUTED DIHYDROBENZOTHIEPINO, DIHYDROBENZOXEPINO AND TETRAHYDRO BENZOCYCLOHEPTA INDOLES AS SELECTIVE ESTROGEN RECEPTOR MODULATORS<br/>[FR] NOUVEAUX DIHYDROBENZOTHIEPINO, DIHYDROBENZOXEPINO ET TETRAHYDRO BENZOCYCLOHEPTA INDOLES N-SUBSTITUES UTILISES EN TANT QUE MODULATEURS DU RECEPTEUR DES OESTROGENES
    申请人:COUNCIL SCIENT IND RES
    公开号:WO2005094833A1
    公开(公告)日:2005-10-13
    The invention provides a novel class of N-substituted dihydrobenzothiepino, dihydrobenzoxepino and tetrahydro benzocyclohepta indoles of Formula (I) and their pharmaceutically acceptable salts, and methods for of synthesizing these compounds. The invention further comprises pharmaceutical compositions and methods of use for these compounds for the treatment of estrogen related diseases or disorders.
    这项发明提供了一类新型的Formula (I)的N-取代二氢苯并噻吩、二氢苯并氧吩和四氢苯并环庚哌啉以及它们的药用盐,以及合成这些化合物的方法。该发明还包括用于治疗雌激素相关疾病或紊乱的这些化合物的药用组合物和使用方法。
  • [EN] TARGETED DRUG DELIVERY THROUGH AFFINITY BASED LINKERS<br/>[FR] ADMINISTRATION CIBLÉE D'UN MÉDICAMENT FAISANT APPEL À DES COUPLEURS FONDÉS SUR L'AFFINITÉ
    申请人:INVICTUS ONCOLOGY PVT LTD
    公开号:WO2015148126A1
    公开(公告)日:2015-10-01
    The current invention discloses targeted drug delivery conjugates comprising a targeting moiety linked to a drug via a molecule having an affinity for the targeting moiety. Typically, the conjugate comprises a targeting ligand and a molecule of interest, e.g., a therapeutic agent. The targeting ligand and the molecule of interest are linked to each other via an affinity ligand. The affinity ligand is further covalently or non-covalently linked to a drug or therapeutic agent. The drug can be modified to make it more soluble and so that it cleaves from the linking molecule at the target site.
    当前的发明揭示了包括通过具有与靶向基团亲和力的分子连接到药物的靶向药物传递共轭物。通常,该共轭物包括一个靶向配体和一个感兴趣的分子,例如,一个治疗剂。靶向配体和感兴趣的分子通过一个亲和配体相互连接。该亲和配体进一步以共价或非共价方式连接到药物或治疗剂。药物可以被修改以使其更溶解,并使其在靶点处从连接分子中解离。
  • COMBINATION THERAPY OF A HIF-2-ALPHA INHIBITOR AND AN IMMUNOTHERAPEUTIC AGENT AND USES THEREOF
    申请人:PELOTON THERAPEUTICS, INC.
    公开号:US20180140569A1
    公开(公告)日:2018-05-24
    The present invention provides methods and pharmaceutical compositions for treating proliferative disorders. The method involves step of administering to said subject a HIF-2alpha inhibitor and an immunotherapeutic agent.
    本发明提供了治疗增殖性疾病的方法和药物组合物。该方法涉及向所述受试者施用HIF-2alpha抑制剂和免疫治疗药物的步骤。
  • [EN] 3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR<br/>[FR] MODULATEURS ALLOSTÉRIQUES DE TYPE 3-(1H-PYRAZOL-4-YL)PYRIDINE DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE
    申请人:MERCK SHARP & DOHME
    公开号:WO2019005588A1
    公开(公告)日:2019-01-03
    The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    本发明涉及吡唑并[4,3-b]吡啶化合物,其为M4毒蕈碱型乙酰胆碱受体的变构调节剂。本发明还涉及在可能治疗或预防神经和精神障碍以及涉及M4毒蕈碱型乙酰胆碱受体的疾病中使用所述化合物。本发明还涉及包含这些化合物的组合物。本发明还涉及在可能预防或治疗涉及M4毒蕈碱型乙酰胆碱受体的疾病中使用这些组合物。
  • SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE10A)
    申请人:Leblond Bertrand
    公开号:US20120214837A1
    公开(公告)日:2012-08-23
    The invention relates to compounds of the formula wherein R′, R 1 , through R 7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    本发明涉及具有以下公式的化合物 其中R',R1,到R7和Ar如本文所述定义。这些化合物作为磷酸二酯酶10(PDE10A)的抑制剂,可用于治疗中枢神经系统疾病,如精神疾病,也可用于治疗例如肥胖、2型糖尿病、代谢综合征、葡萄糖不耐受、疼痛和眼科疾病。
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